The Sonoran Desert Toad

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Bufo alvarius

Search History for bufo alvarius returned 24 records in BIOSIS Previews 7/2003:

TI: Hypoglossal sensory afferents facilitate ballistic tongue protraction in Bufo alvarius.
AU: Desrochers-D-M {a}; Nishikawa-K-C {a}
AD: {a} Northern Arizona University, Flagstaff, AZ, USA
SO: American-Zoologist. [print] December, 2001; 41 (6): 1426-1427.
PY: 2001
DT: Meeting-
IS: 0003-1569
MT: Annual Meeting of the Society for Integrative and Comparative Biology, Anaheim, California, USA, January 02-06, 2002
LA: English
AB: Toads of the Genus Bufo protract the tongue in a ballistic manner during prey capture. Kinematics analyses have shown the tongue of the toad Bufo alvarius moving with maximum velocities greater than 2 m/s and accelerations exceeding 1000 m/s2 during feeding. One goal of this study is to elucidate how B. alvarius is able to catapult the tongue out of the mouth with such large velocities and accelerations. I suggest that the tongue is spring-loaded in the mouth prior to mouth opening. While the tongue is rolled forward towards its anterior attachment point, the mouth-opening muscles (depressors) and mouth-closing muscles (levators) fire simultaneously, and the mouth remains closed. Then, a signal reaches the levators, inactivating both the tonic and phasic elements of these muscles and allowing the depressors to open the mouth at high velocity. As the lower jaw drops down, the tongue is thrown out over the lower jaw tip with a straight-line anterior trajectory. Once the tongue tip has passed over the lower jaw tip, inertia carries the tongue to maximum protraction. Via this mechanism, the tongue able to exit the mouth with great velocities and accelerations, enabling it to lengthen as it is protracted. In order for this mechanism of tongue protraction to operate, the movements of the tongue and jaws must be precisely coordinated. The paired hypoglossal nerves facilitate this coordination. Proprioceptive information about the tongue, carried by hypoglossal afferents, is used to modulate the activity of the jaw levators. Further, both hypoglossal afferents must be operational in order for the ballistic mechanism to produce maximum tongue protraction.
AI: Y
MC: Dental-and-Oral-System (Ingestion-and-Assimilation); Muscular-System (Movement-and-Support); Nervous-System (Neural-Coordination)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-): toad-
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
PS: depressor-muscles: muscular-system; hypoglossal-nerves: nervous-system; jaws-: dental-and-oral-system; levator-muscles: muscular-system; mouth-: dental-and-oral-system; tongue-: dental-and-oral-system, protraction-
MQ: kinematics-analysis: analytical-method
MI: acceleration-; feeding-; prey-capture; tongue-velocity; Meeting-Abstract
AN: 200200464897
UD: 20020829


TI: Scaling of the feeding mechanism in the Colorado River toad.
AU: McGowan-C-P {a}; O'-Reilly-J-C {a}; Nishikawa-K-C {a}
AD: {a} Northern Arizona University, Flagstaff, AZ, USA
SO: American-Zoologist. [print] December, 2000; 40 (6): 1125.
PY: 2000
DT: Meeting-
IS: 0003-1569
MT: Annual Meeting and Exhibition of the Society for Integrative and Comparative Biology, Chicago, Illinois, USA, January 03-07, 2001
LA: English
LS: English
AB: There are several potential structural and functional consequences of an animal changing size. As the whole animal grows, individual components that make up complex functional systems, such as the feeding mechanism, may grow at varying rates. To explore this issue, we examined the feeding system of the Colorado River Toad, Bufo alvarius, modeled as a simple mechanical lever system. We evaluated several aspects of the feeding mechanism, including skull measurements, linear jaw measurements, mechanical advantage of jaw opening and closing, jaw opening and closing musculature and in vivo bite forces. Components of the feeding system were scaled against body length in order to test for isometry and establish relative growth rates. The sample size included 30 animals ranging from 15 to 130 mm in body length as well as a separate group of 12 live toads in this size range, which were used to acquire bite forces. The results of the changing skull and jaw morphology were related to existing feeding kinematics for Bufo alvarius of a similar size range. Mechanical advantage remained constant for both jaw opening and closing, though the lever arms measured to determine mechanical advantage were not isometric with respect to body size. The predicted jaw Closing force was very similar to that observed in vivo, but also did not scale isometrically with size. The results of the predicted jaw Opening forces however did not match that observed through kinematics, suggesting that some other component not explored in this study is active in the ballistic tongue protraction mechanism of this species.
AI: Y
MC: Models-and-Simulations (Computational-Biology); Dental-and-Oral-System (Ingestion-and-Assimilation)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius [Colorado-River-toad] (Salientia-)
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
PS: jaw-: dental-and-oral-system, musculature-, skeletal-system; skull-: skeletal-system; tongue-: ballistic-contraction, dental-and-oral-system
MI: bite-forces: closing-, opening-; body-length; body-size-scaling; feeding-mechanisms; isometry-; kinematics-; Meeting-Abstract
AN: 200100373200
UD: 20010806


TI: Hypoglossal sensory feedback control during feeding in the toad, Bufo alvarius.
AU: Desrochers-D-M {a}; Nishikawa-K-C {a}
AD: {a} Northern Arizona University, Flagstaff, AZ, USA
SO: American-Zoologist. [print] December, 2000; 40 (6): 996.
PY: 2000
DT: Meeting-
IS: 0003-1569
MT: Annual Meeting and Exhibition of the Society for Integrative and Comparative Biology, Chicago, Illinois, USA, January 03-07, 2001
LA: English
LS: English
AB: This study explores the role of hypoglossal sensory feedback during feeding in the toad Bufo alvarius. Prior studies indicate that sensory feedback from the hypoglossal nerves can trigger inhibition of both tonic and phasic activity of the jaw levator muscles. Temporary inhibition of the jaw levators allows the jaw depressors to produce rapid mouth opening. Following bilateral hypoglossal transection, the levators and depressors fire simultaneously, preventing mouth opening during feeding attempts. Utilizing unilateral rather than bilateral hypoglossal transections, coupled with high-speed digital videography and EMG recordings from the jaw levators and depressors, I have further investigated hypoglossal feedback control of the anuran jaw musculature. Preliminary data show that while the mouth opens following unilateral transection, the velocity of mouth opening and the maximum gape angle are reduced. These results suggest that transection of the hypoglossal nerve on one side prevents the inhibition of tonic and phasic activity of the jaw levators only on that same side. Hence, on that side of the jaw, the levators and depressors may be firing simultaneously, resisting the efforts of the contralateral depressors to open the mouth and therefore reducing the speed and maximum gape angle of mouth opening. According to this scenario, each hypoglossal nerve carries information back to the central nervous system in a unilateral fashion. Nerve staining studies are currently being conducted to further test this hypothesis.
AI: Y
MC: Behavior-; Dental-and-Oral-System (Ingestion-and-Assimilation); Nervous-System (Neural-Coordination)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-): toad-
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
PS: hypoglossal-nerve: nervous-system; jaw-: dental-and-oral-system, skeletal-system; jaw-levator-muscles: muscular-system; mouth-: dental-and-oral-system, opening-
MQ: electromyography-: analytical-method; high-speed-digital-videography: analytical-method
MI: feeding-; sensory-feedback; Meeting-Abstract
AN: 200100349790
UD: 20010717


TI: The spinal nerves innervate putative chemosensory cells in the ventral skin of desert toads, Bufo alvarius.
AU: Koyama-Hiromichi; Nagai-Takatoshi {a}; Takeuchi-Hiro-aki; Hillyard-Stanley-D
AD: {a} Department of Biology, Keio University School of Medicine, Hiyoshi 4-1-1, Kouhoku-ku, Yokohama, 223-8521, Japan
SO: Cell-and-Tissue-Research. [print] May, 2001; 304 (2): 185-192.
PY: 2001
DT: Article-
IS: 0302-766X
LA: English
LS: English
AB: Toads normally obtain water by absorption across their skin from osmotically dilute sources. When hyperosmotic salt solutions are presented as a hydration source to dehydrated desert toads, they place the ventral skin onto the source but soon afterwards escape to avoid dehydration. The escape behavior coincides with neural excitation of the spinal nerves that innervate putative chemosensory cells in the ventral skin. In the present study, fluorescent dye translocated through the spinal nerves to those receptor cells in the epidermis was photoconverted in the presence of 3, 3'-diaminobenzidine tetrahydrochloride for electron-microscopic observation of the cells and associated nerve terminals. Most of the photoconverted cells were located in the deepest layer of the epidermis, with some being in more intermediate layers. No labeled cell was seen in the outermost layer of living cells. In desert toads, flask cells and Merkel cells are occasionally seen in the epidermis. An association of nerve fibers with these epidermal cells has been reported in some species of the anurans. In the present study, however, the cytological features of the photoconverted cells are neither reminiscent of flask cells nor Merkel cells, but are similar to those of surrounding epithelial cells in each layer of the epidermis. We hypothesize a sensory function for these cells, because they have a close association with nerve fibers and participate in the transepithelial transport of salts that must pass through all cell layers of the skin.
AI: Y
MC: Integumentary-System (Chemical-Coordination-and-Homeostasis); Nervous-System (Neural-Coordination)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius [desert-toad] (Salientia-)
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
PS: Merkel-cells: nervous-system; chemosensory-cells: sensory-system; epidermis-: integumentary-system; flask-cells; spinal-nerves: nervous-system; ventral-skin: integumentary-system
AN: 200100307889
UD: 20010619


TI: Immunohistochemical study amiloride-sensitive Na+ channel in the skin of anuran amphibian.
AU: Torii-Y {a}; Kanazashi-K {a}; Takeuchi-H-A {a}; Kasai-M; Takada-M; Nagai-T
AD: {a} Dept. of Biol., Fac. of Sci., Shizuoka Univ., Shizuoka, Japan
SO: Zoological-Science-Tokyo. [print] December, 2000; 17 (Supplement): 93.
PY: 2000
DT: Meeting-
IS: 0289-0003
MT: Seventy-First Annual Meeting of the Zoological Society of Japan, Yamagata, Japan, September 21-23, 2000
LA: English
LS: English
MC: Integumentary-System (Chemical-Coordination-and-Homeostasis); Urinary-System (Chemical-Coordination-and-Homeostasis); Physiology-
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius [desert-toad] (Salientia-); Hyla-arborea-japonica [tree-frog] (Salientia-); Rana-catesbeiana [bullfrog-] (Salientia-); Xenopus-sp. (Salientia-): anuran-amphibian
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
PS: renal-tubule: excretory-system; skin-granular-cell-layers: integumentary-system
CB: biotin-; sodium-ion-channel: amiloride-sensitive
RN: 58-85-5: BIOTIN
MQ: immunohistochemistry-: Immunohistochemical/Immunocytochemical-Techniques, histochemical-method, immunologic-method
MI: mesic-environment; xeric-habitat; Meeting-Abstract
AN: 200100262953
UD: 20010521

TI: Chemosensory function of the ventral skin in the desert toads.
AU: Nagai-Takatoshi {a}
AD: {a} Department of Physiology, Teikyo University School of Medicine, Kaga 2-11-1, Itabashi-ku, Tokyo, 173-8605, Japan
SO: Pfluegers-Archiv-European-Journal-of-Physiology. 2000; 439 (3 Suppl.): R200.
PY: 2000
DT: Meeting-
IS: 0031-6768
MT: 1998 Life Sciences Conference: Signalling Concepts in Life Sciences., Godz Martuljek, Slovenia, September 19-24, 1998
LA: English
LS: English
MC: Biochemistry-and-Molecular-Biophysics; Integumentary-System (Chemical-Coordination-and-Homeostasis); Nervous-System (Neural-Coordination); Sensory-Reception
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius [desert-toad] (Salientia-)
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
PS: skin-: chemosensory-function, integumentary-system, osmotic-water-flow, ventral-; spinal-nerves: nervous-system
CB: amiloride-; potassium-chloride; sodium-chloride
RN: 2609-46-3: AMILORIDE; 7447-40-7: POTASSIUM CHLORIDE; 7647-14-5: SODIUM CHLORIDE
MI: Meeting-Abstract
AN: 200000242287
UD: 20000606


TI: Buccal oscillation behavior and body size in the Sonoran Desert toad (Bufo alvarius).
AU: Choquette-D-M {a}; O'-Reilly-J-C {a}; Brainerd-E-L {a}
AD: {a} Univ. of Massachusetts, Amherst, MA, USA
SO: American-Zoologist. 1999; 39 (5): 81A.
PY: 1999
DT: Meeting-
IS: 0003-1569
MT: Annual Meeting of the Society for Integrative and Comparative Biology., Atlanta, Georgia, USA, January 04-08, 2000
SP: Society for Integrative and Comparative Biology
LA: English
LS: English
MC: Physiology-
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius [Sonoran-desert-toad] (Salientia-)
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
MI: body-size; buccal-oscillation-behavior; Meeting-Abstract
AN: 200000187119
UD: 20000512


TI: Scaling in the skull of the Colorado River toad, Bufo alvarius.
AU: McGown-C-P {a}; O'-Reilly-J-C {a}; Birch-J-M {a}; Nishikawa-K-C {a}
AD: {a} Northern Arizona Univ., Flagstaff, AZ, USA
SO: American-Zoologist. 1999; 39 (5): 96A.
PY: 1999
DT: Meeting-
IS: 0003-1569
MT: Annual Meeting of the Society for Integrative and Comparative Biology., Atlanta, Georgia, USA, January 04-08, 2000
SP: Society for Integrative and Comparative Biology
LA: English
LS: English
MC: Skeletal-System (Movement-and-Support)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius [Colorado-River-toad] (Salientia-)
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
PS: jaw-; skull-
MI: body-size; isometric-feeding-kinematics; movement-kinematics; Meeting-Abstract
AN: 200000185201
UD: 20000512


TI: The epithelial cells with spinal innervation in the chemosensory ventral skin of desert toads.
AU: Nagai-T {a}; Koyama-H; Hillyard-S-D
AD: {a} Dept. Physiol., Teikyo Univ. Sch. Med., Tokyo, Japan
SO: Zoological-Science-Tokyo. Dec., 1999; 16 (Suppl.): 99.
PY: 1999
DT: Meeting-
IS: 0289-0003
MT: 70th Annual Meeting of the Zoological Society of Japan., Yamagata, Japan, September 27-29, 1999
SP: Zoological Society of Japan
LA: English
LS: English
MC: Chemical-Coordination-and-Homeostasis; Integumentary-System (Chemical-Coordination-and-Homeostasis)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-)
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
PS: Merkel-cells: mechanosensory-, nervous-system; epithelial-cells; spinal-nerves: nervous-system; stratum-basale: integumentary-system; ventral-skin: chemosensory-, integumentary-system
MQ: electron-microscopy: examination-method
MI: cell-distribution; chemical-stimuli; chemosensory-transduction; escape-behavior; nerve-response-latency; osmotic-flow; spinal-innervation; Meeting-Abstract
AN: 200000154867
UD: 20000418


TI: Breeding activity, estimated age-structure, and growth in Sonoran Desert anurans.
AU: Sullivan-Brian-K {a}; Fernandez-Philip-J
AD: {a} Department of Life Sciences, Arizona State University West, Phoenix, AZ, 85069, USA
SO: Herpetologica-. Sept., 1999; 55 (3): 334-343.
PY: 1999
DT: Article-
IS: 0018-0831
LA: English
LS: English
AB: We investigated breeding activity of a community of desert anurans at two sites in north-central Phoenix, Maricopa County, Arizona, during 1990-1995. Four species used these sites for breeding during the summer monsoon season: Colorado River toad, Bufo alvarius, Great Plains toad, B. cognatus, red-spotted toad, B. punctatus, and Couch's spadefoot toad, Scaphiopus couchii. Breeding activity was restricted primarily to 1990 and 1992 when significant rainfall events (>25 mm of rainfall within 24 h) occurred repeatedly. No breeding (i.e., oviposition) occurred during 1991 or 1993, and only S. couchii bred on a single night in 1994 and B. alvarius on a single night in 1995. We undertook a skeletochronologic analysis of lines of arrested growth in digits and femurs with all four study species. Conservative estimates of age based on lines of arrested growth (LAG's) suggest that populations of all four taxa were relatively young (average age between two and four years) at both sites in 1994 and 1995. Growth, as indicated by the amount of bone deposited between LAG's, was greatest during the second year in B. alvarius and B. cognatus, but not B. punctatus or S. couchii. These results indicate rapid growth to maturity but do not support the notion that these anuran amphibians are long-lived organisms that exhibit an extended reproductive lifespan as adults in response to a highly variable, harsh desert environment.
AI: Y
MC: Population-Studies; Terrestrial-Ecology (Ecology-, Environmental-Sciences)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius [Colorado-River-toad] (Salientia-); Bufo-cognatus [Great-Plains-toad] (Salientia-); Bufo-punctatus [red-spotted-toad] (Salientia-); Scaphiopus-couchii [Couch's-spadefoot-toad] (Salientia-)
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
GE: Phoenix- (Arizona-, USA-, North-America, Nearctic-region); Sonoran-Desert (North-America, Nearctic-region)
MQ: skeletochronological-analysis: analytical-method
MI: age-structure; breeding-; calling-behavior; growth-; rainfall-event; reproductive-lifespan
AN: 199900504726
UD: 19991117

TI: Natural hybridization among distantly related toads (Bufo alvarius, Bufo cognatus, Bufo woodhousii) in Central Arizona.
AU: Gergus-Erik-W-A {a}; Malmos-Keith-B; Sullivan-Brian-K
AD: {a} Department of Zoology, Arizona State University, Tempe, AZ, 85287-1501, USA
SO: Copeia-. May, 1999; 199 (2): 281-286.
PY: 1999
DT: Article-
IS: 0045-8511
LA: English
LS: English
AB: Putative hybrid toads of the genus Bufo were collected in central Arizona and identified using allozymes, qualitative and quantitative morphological characters, and release call characteristics. Data suggest one hybrid resulted from mating between Bufo cognatus and Bufo woodhousii, and the other three resulted from matings between Bufo alvarius and B. woodhousii. Natural hybridization between these taxa has not been previously reported. To date, B. woodhousii has been found to hybridize with four species of the Bufo americanus species group, of which B. woodhousii is a member, and five other species which represent three outgroups to the B. americanus group. Fossil evidence suggests some genomic compatability has been retained between B. alvarius and B. woodhousii despite at least 6 million years of independent evolution. Hybridization among members of Bufo may be due to alternative mating tactics of males, such as active searching, and by alteration of historicalhabitats in central Arizona.
AI: Y
MC: Evolution-and-Adaptation; Population-Genetics (Population-Studies)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-); Bufo-cognatus (Salientia-); Bufo-woodhousii (Salientia-)
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
CB: allozymes-
MI: genomic-compatibility; habitat-disturbance; hybridization-; mating-; morphology-
AN: 199900277088
UD: 19990709

TI: Development of feeding behavior in juvenile toads, Bufo alvarius, after metamorphosis from the tadpole stage.
AU: Benally-R; Nishikawa-K-C
AD: Northern Ariz., Univ., Flagstaff, AZ, USA
SO: American-Zoologist. 1998; 38 (5) 200A.
PY: 1998
DT: Meeting-
IS: 0003-1569
MT: Annual Meeting of the Society for Integrative and Comparative Biology, Chicago, Illinois, USA, January 6-10, 1999
LA: English
MC: Behavior-; Development-
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-): juvenile-
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
PS: jaw-: dental-and-oral-system, skeletal-system; tongue-: dental-and-oral-system
MI: feeding-behavior; metamorphosis-; prey-size; Meeting-Abstract
AN: 199900172610
UD: 19990422


TI: Neopalatine odontoids in Bufo alvarius (Anura: Bufonidae).
AU: Mendelson-Joseph-R-III; Pramuk-Jennifer-B {a}
AD: {a} Dep. Syst. Ecol., Univ. Kans., Lawrence, KS 66045-2454, USA
SO: Journal-of-Herpetology. Dec., 1998; 32 (4) 586-588.
PY: 1998
DT: Article-
IS: 0022-1511
LA: English
MC: Skeletal-System (Movement-and-Support)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-): Anura-, Bufonidae-
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
PS: neopalatine-odontoids: skeletal-system; skull-: skeletal-system
MI: feeding-ecology; synapomorphy-
AN: 199900079309
UD: 19990219


TI: The ventral skin epithelium of Colorado River toads.
AU: Koyama-H {a}; Nagai-T
AD: {a} Coll. Nurs., Yokohama City Univ., Yokohoma, Japan
SO: Zoological-Science-Tokyo. Dec., 1997; 14 (SUPPL.) 112.
PY: 1997
DT: Meeting-
IS: 0289-0003
MT: Sixty-Eighth Annual Meeting of the Zoological Society of Japan, Nara, Japan, October 2-4, 1997
SP: Zoological Society of Japan
LA: English
MC: Physiology-
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius [desert-toad] (Salientia-)
TN: Amphibians-; Animals-; Chordates-; Nonhuman-Vertebrates; Vertebrates-
PS: ventral-skin-epithelium: cell-morphology, integumentary-system
MI: Meeting-Abstract
AN: 199800282293
UD: 19980508


TI: Chemosensory function of the ventral skin in Colorado river toads.
AU: Nagai-T {a}; Koyama-H; Hoff-K-V-S; Hillyard-S-D
AD: {a} Dep. Physiology, Teikyo Univ. Sch. Med., Tokyo 173, Japan
SO: Society-for-Neuroscience-Abstracts. 1997; 23 (1-2) 250.
PY: 1997
DT: Meeting-Abstract; Meeting-Poster
IS: 0190-5295
MT: 27th Annual Meeting of the Society for Neuroscience, Part 1, New Orleans, Louisiana, USA, October 25-30, 1997
LA: English
MC: Biochemistry-and-Molecular-Biophysics; Integumentary-System (Chemical-Coordination-and-Homeostasis); Sense-Organs (Sensory-Reception)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-)
TN: amphibians-; animals-; chordates-; nonhuman-vertebrates; vertebrates-
CB: SODIUM-
RN: 7440-23-5: SODIUM
MI: CHEMOSENSORY-FUNCTION; COLORADO-RIVER-TOAD; INTEGUMENTARY-SYSTEM; SENSE-ORGANS; SODIUM-ABSORPTION; STRATUM-GERMINATIVUM; VENTRAL-SKIN
AN: 199799767206


TI: Scaling of the kinematics and motor control of prey capture in salamanders and toads.
AU: Deban-S-M {a}; O'-Reilly-J-C
AD: {a} Univ. Calif., Berkeley, CA, USA
SO: Journal-of-Morphology. 1997; 232 (3) 246.
PY: 1997
DT: Meeting-Abstract
IS: 0362-2525
MT: Fifth International Congress of Vertebrate Morphology, Bristol, England, UK, July 12-17, 1997
LA: English
MC: Dental-and-Oral-System (Ingestion-and-Assimilation); Morphology-; Muscular-System (Movement-and-Support); Physiology-
ST: Caudata-: Amphibia-, Vertebrata-, Chordata-, Animalia-; Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-); Cryptobranchus-alleganiensis (Caudata-)
TN: amphibians-; animals-; chordates-; nonhuman-vertebrates; vertebrates-
MI: BODY-SIZE; FEEDING-MUSCLE; HELLBENDER-; JAW-MUSCLE; KINEMATICS-; MOTOR-PATTERN; MOVEMENT-AND-SUPPORT; MUSCULAR-SYSTEM; PREY-CAPTURE
AN: 199799626597


TI: Novel sensory receptors involved in the water absorption behavior of desert toads.
AU: Nagai-T {a}; Koyama-H; Hillyard-S-D
AD: {a} Dep. Physiol., Teikyo Univ. Sch. Med., Tokyo, Japan
SO: Zoological-Science-Tokyo. 1996; 13 (SUPPL.) 112.
PY: 1996
DT: Meeting-Abstract
IS: 0289-0003
MT: Sixty-seventh Annual Meeting of the Zoological Society of Japan, Sapporo, Japan, September 18-20, 1996
LA: English
MC: Biochemistry-and-Molecular-Biophysics; Cell-Biology; Integumentary-System (Chemical-Coordination-and-Homeostasis)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-)
TN: amphibians-; animals-; chordates-; nonhuman-vertebrates; vertebrates-
MI: DESSERT-TOAD; INTEGUMENTARY-SYSTEM; SENSORY-RECEPTORS; SKIN-; WATER-ABSORPTION-RESPONSE
AN: 199799489242


TI: The scaling of feeding kinematics in toads (Anura: Bufonidae).
AU: O'-Reilly-J-C; Lindstedt-S-L; Nishikawa-K-C
AD: Northern Ariz. Univ., AZ, USA
SO: American-Zoologist. 1993; 33 (5) 147A.
PY: 1993
DT: Meeting-
IS: 0003-1569
MT: Annual Meeting of the American Society of Zoologists, Los Angeles, California, USA, December 26-30, 1993
LA: English
MC: Behavior-; Morphology-; Nutrition-; Physiology-
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-)
TN: amphibians-; animals-; chordates-; nonhuman-vertebrates; vertebrates-
MI: BODY-SIZE; MEETING-ABSTRACT; MOVEMENTS-; PREY-CAPTURE
AN: 199497383451


TI: Call variation in the Colorado River toad (Bufo alvarius): Behavioral and phylogenetic implications.
AU: Sullivan-Brian-K {a}; Malmos-Keith-B
AD: {a} Life Sciences Prog., P.O. Box 37100, Arizona State Univ. West, Phoenix, AZ 85069-7100, USA
SO: Herpetologica-. 1994; 50 (2) 146-156.
PY: 1994
DT: Article-
IS: 0018-0831
LA: English
AB: We studied variation in advertisement calls, release calls, and calling behavior in three populations of Bufo alvarius in central Arizona over a 3-yr period. Of advertisement call variables, pulse rate was the only variable significantly (positively) related to temperature, and no variables were correlated with male snout-vent length. For release calls only pulse rate was significantly (negatively) related to temperature, and no variables were related to male size. Mean advertisement call pulse rate was approximately 30% of average release call pulse rate; such dramatic differences in temporal structure of advertisement and release calls are previously unreported in the genus Bufo. These results support the hypothesis that B. alvarius generates advertisement calls without passive vibrations of the arytenoid cartilages. Overall patterns of call variation in B. alvarius more closely parallel the valliceps rather than the boreas species group. Preliminary discrimination trials indicate that females are attracted to malt, advertisement calls. Within relatively low density choruses, some large males produced advertisement calls consistently, and active-searching behavior was size-related. Male advertisement calls may play an important role in mate selection by females under some conditions, but an adequate test of this hypothesis awaits additional study.
AI: Y
MC: Behavior-; Evolution-and-Adaptation; Freshwater-Ecology (Ecology-, Environmental-Sciences); Reproductive-System (Reproduction-)
ST: Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-)
TN: amphibians-; animals-; chordates-; nonhuman-vertebrates; vertebrates-
MI: ADVERTISEMENT-CALL; EVOLUTION-; MATE-SELECTION; RELEASE-CALL; REPRODUCTIVE-BEHAVIOR
AN: 199497354697


TI: Bufo alvarius: A potent hallucinogen of animal origin.
AU: Weil-Andrew-T {a}; Davis-Wade
AD: {a} College Med., Univ. Arizona, Tucson, AZ 85724, USA
SO: Journal-of-Ethnopharmacology. 1994; 41 (1-2) 1-8.
PY: 1994
DT: Article-
IS: 0378-8741
LA: English
AB: Anthropologists have long speculated that ancient peoples of Mesoamerica used a toad, Bufo marinus, as a ritual intoxicant. This hypothesis rests on many iconographic and mythological representations of toads and on a number of speculative ethnographic reports. The authors reject B. marinus as a candidate for such use because of the toxicity of its venom. A more likely candidate is the Sonoran desert toad, Bufo alvarius, which secretes large amounts of the potent known hallucinogen, 5-methoxy-NN-dimethyltryptamine (5-MeO-DMT). The authors demonstrate that the venom of B. alvarius, although known to be toxic when consumed orally, may be safely smoked and is powerfully psychoactive by that route of administration. These experiments are the first documentation of an hallucinogenic agent from the animal kingdom, and they provide clear evidence of a psychoactive toad that could have been employed by Precolumbian peoples of the New World.
AI: Y
MC: Anthropology-; Biochemistry-and-Molecular-Biophysics; Dental-and-Oral-System (Ingestion-and-Assimilation); History-; Human-Ecology (Anthropology-); Methods-and-Techniques; Paleobiology-; Pharmacognosy- (Pharmacology-); Pharmacology-; Respiratory-System (Respiration-); Toxicology-
ST: Aves-Unspecified: Aves-, Vertebrata-, Chordata-, Animalia-; Hominidae-: Primates-, Mammalia-, Vertebrata-, Chordata-, Animalia-; Insecta-Unspecified: Insecta-, Arthropoda-, Invertebrata-, Animalia-; Pisces-Unspecified: Pisces-, Vertebrata-, Chordata-, Animalia-; Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: bird- (Aves-Unspecified); fish- (Pisces-Unspecified); human- (Hominidae-); insect- (Insecta-Unspecified); Aves- (Aves-Unspecified); Bufo-alvarius (Salientia-); Bufo-marinus (Salientia-); Insecta- (Insecta-Unspecified); Pisces- (Pisces-Unspecified)
TN: amphibians-; animals-; arthropods-; birds-; chordates-; fish-; humans-; insects-; invertebrates-; mammals-; nonhuman-vertebrates; primates-; vertebrates-
CB: 5-METHOXY-N,N-DIMETHYLTRYPTAMINE
TM: Archean-
RN: 1019-45-0: 5-METHOXY-N,N-DIMETHYLTRYPTAMINE
MI: ANCIENT-MESOAMERICA; ARCHAEOLOGICAL-EVIDENCE; ETHNOGRAPHY-; GLOBAL-OCCURRENCES; ICONOGRAPHY-; INTAKE-MODE; MYTHOLOGY-; ORAL-INGESTION; PRECOLUMBIAN-USE; PSYCHOACTIVE-AGENTS; SMOKING-; TOAD-VENOM; TOXICITY-; 5-METHOXY-N,N-DIMETHYLTRYPTAMINE
AN: 199497243190


TI: HELMINTHS OF THREE TOADS BUFO-ALVARIUS BUFO-COGNATUS BUFONIDAE AND SCAPHIOPUS-COUCHII PELOBATIDAE FROM SOUTHERN ARIZONA USA.
AU: GOLDBERG-S-R {a}; BURSEY-C-R
AD: {a} DEP BIOL, WHITTIER COLLEGE, WHITTIER, CALIF 90608
SO: Journal-of-the-Helminthological-Society-of-Washington. 1991; 58 (1): 142-146.
PY: 1991
DT: Article-
IS: 1049-233X
LA: ENGLISH
AB: The gastrointestinal tracts and lungs of 3 toad species were examined for helminths. Examination of 95 Bufo alvarius revealed the presence of the nematodes Aplectana itzocanensis Bravo Hollis, 1943, Physaloptera sp. Rudolphi, 1819, Physocoephalus sp. Diesting, 1861, Oswaldocruzia pipiens Walton, 1929, the cestode Nematotaenia dispar (Goeze, 1782) Luhe, 1899, in the gastrointestinal tract, and the nematode Rhabdias americanus Baker, 1978, in the lungs. Bufo cognatus (N = 21) had the nematodes A. itzocanensis, O. pipiens, Physaloptera sp., and the cestode Distoichometra bufonis Dickey, 1921, in the gastrointestinal tract. The nematode R. americanus was found in the lungs. Scaphiopus couchii (N = 76) had the nematodes Aplectana incerta Caballero, 1949 and O. pipiens, and the cestode D. bufonis in the digestive trace. No helminths were found in the lungs of S. couchii.
AI: Y
ST: Cestoda-: Platyhelminthes-, Helminthes-, Invertebrata-, Animalia-; Nematoda-: Aschelminthes-, Helminthes-, Invertebrata-, Animalia-; Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
TN: Amphibians-; Animals-; Aschelminths-; Chordates-; Helminths-; Invertebrates-; Nonhuman-Vertebrates; Platyhelminths-; Vertebrates-
MI: APLECTANA-ITZOCANENSIS APLECTANA-INCERTA PHYSALOPTERA-SP PHYSOCEPHALUS-SP OSWALDOCRUZIA-PIPIENS NEMATOTAENIA-DISPAR RHABDIAS-AMERICANUS DISTOICHOMETRA-BUFONIS GASTROINTESTINAL TRACT LUNG PARASITISM
AN: 199191122016
UD: 1991


TI: THE SANGAMON INTERGLACIAL VERTEBRATE FAUNA FROM RANCHO-LA-BRISCA SONORA MEXICO.
AU: VAN-DEVENDER-T-R {a}; REA-A-M; SMITH-M-L
AD: {a} ARIZ SONORA DESERT MUSEUM, ROUTE 9, BOX 900, TUCSON, AZ 85743, USA
SO: Transactions-of-the-San-Diego-Society-of-Natural-History. 1985 (RECD. 1986); 21 (2): 23-55.
PY: 1985 (RECD 1986)
DT: Article-
IS: 0080-5947
LA: ENGLISH
AB: Bones of 51 species of vertebrates including fish, amphibians, reptiles, birds, and mammals were recovered from a sedimentary deposit at Rancho la Brisca in north-central Sonora, Mexico. The fauna was preserved in a marshy cienega habitat with 49.0% of the species and 87.2% of the identified bones representing aquatic and semiaquatic animals. The most common animals in the fauna are Kinosternon sonoriense (Sonoran Mud Turtle) and Rana "pipiens:-complex (Leopard Frog). The presence of Bison species (Bison) in association with Mammuthus species (Mammoth), Equus cf. tau (Pygmy Onager), and Camelops species (Camel) places the fauna in the Rancholabrean Land Mammal Age. Bufo cf. kelloggi (Little Mexican Toad), B. mazatlanensis (Sinaloa Toad), Leptodactylus melanonotus (Sabinal Frog), pternohyla fodiens (Burrowing Treefrog), and Masticophis cf. mentovarius (Tropical Whipsnake) are subtropical thornscrub or Sonoran Desert animals that presently occur to the south and/or west of la Brisca. Bufo alvarus (Colorado River Toad), cf. Callisaurus draconoides (Zebra-tailed Lizard), and Sceloporus cf. clarkii (Clark's Spiny Lizard) are other Sonoran Desert animals that suggest a paleoclimate with warm winters and a well-developed summer monsoon. The best modern analog for the paleocommunity would be about 240 km SSE on the Rio Yaqui. The subtropical elements in the la Brisca fauna make it unlikely that the fauna was deposited during a glacial period, considering that the Late Wisconsin paleoclimatic reconstructions for Arizona [USA] based on plant remains in packrat middens suggest glacial climates with mild, wet winters and cool, dry summers. The fauna represents an interglacial environment subsequent to the appearance of Bison about 150 000 years ago in the Sangamon Interglacial and with a climate to that of the Late Holocene of the last 4000 years. The distributions of fish and mud turtles suggest past stream connections between the Gila River drainage in southeastern Arizona and the rivers in Sonora. In contrast, Pseudemys scripta (Yaqui Slider) apparently never entered Arizona, although it reaches north-central Sonora today.
AI: Y
ST: Pisces-: Vertebrata-, Chordata-, Animalia-; Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-; Chelonia-: Reptilia-, Vertebrata-, Chordata-, Animalia-; Sauria-: Reptilia-, Vertebrata-, Chordata-, Animalia-; Aves-: Vertebrata-, Chordata-, Animalia-; Bovidae-: Artiodactyla-, Mammalia-, Vertebrata-, Chordata-, Animalia-; Camelidae-: Artiodactyla-, Mammalia-, Vertebrata-, Chordata-, Animalia-; Equidae-: Perissodactyla-, Mammalia-, Vertebrata-, Chordata-, Animalia-; Elephantidae-: Proboscidea-, Mammalia-, Vertebrata-, Chordata-, Animalia-
TN: Amphibians-; Animals-; Artiodactyls-; Birds-; Chordates-; Elephants-; Fish-; Mammals-; Nonhuman-Mammals; Nonhuman-Vertebrates; Perissodactyls-; Reptiles-; Vertebrates-
MI: KINOSTERNON-SONORIENSE RANA-PIPIENS BISON MAMMUTHUS EQUUS-TAU CAMELOPS BUFO-KELLOGGI BUFO-MAZATLANENSIS BUFO-ALVARIUS LEPTODACTYLUS-MELANONOTUS SCELOPORUS-CLARKII PTERNOHYLA-FODIENS MASTICOPHIS-MENTOVARIUS CAULISAURUS-DRACONOIDES PSEUDEMYS-SCRIPTA FISH BIRD SEASONALITY PALEOCLIMATE HOLOCENE PLEISTOCENE ARIZONA USA
AN: 198681084900
UD: 1986


TI: 4 NORLEUCINE-7-D-PHENYLALANINE ALPHA MSH A SUPERPOTENT MELANOTROPIN WITH PROLONGED ACTION ON VERTEBRATE CHROMATOPHORES.
AU: HADLEY-M-E {a}; MIEYR-J-H; MARTIN-B-E; CASTRUCCI-A-M-D-L; HRUBY-V-J; SAWYER-T-K; POWERS-E-A; RAO-K-R
AD: {a} DEP ANATOMY AND MOLECULAR, UNIV ARIZONA, TUCSON, AZ 85724
SO: Comparative-Biochemistry-and-Physiology-A. 1985; 81 (1): 1-6.
PY: 1985
DT: Article-
IS: 0300-9629
LA: ENGLISH
AB: The in vitro and in vivo responses of integumental chromatophores to .alpha.-MSH and a related analog, [Nle4, D-Phe7]-.alpha.-MSH, were studied in a number of vertebrate species: the teleost, Lebistes reticulatus; the amphibians, Rana pipiens. R. catesbeiana, Xenopus laevis, Bufo alvarius and B. cognatus; the lizard, Anolis carolinensis; the rattlesnake, Crotalus atrox. The .alpha.-MSH analog was a superpotent agonist in the in vitro frog (R. pipiens, R. catesbeiana) and lizard (A. carolinensis) skin bioassays. In all species studied, the analog exhibited ultraprolonged melanotropic activity, both in vitro and in vivo. This MSH and related analogs should prove useful in the study of numerous physiological processes, particularly when prolonged melanotropic activity is desired.
AI: Y
ST: Osteichthyes-: Pisces-, Vertebrata-, Chordata-, Animalia-; Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-; Sauria-: Reptilia-, Vertebrata-, Chordata-, Animalia-; Serpentes-: Reptilia-, Vertebrata-, Chordata-, Animalia-
TN: Amphibians-; Animals-; Chordates-; Fish-; Nonhuman-Vertebrates; Reptiles-; Vertebrates-
MI: LEBISTES-RETICULATUS RANA-PIPIENS RANA-CATESBEIANA XENOPUS-LAEVIS BUFO-ALVARIUS BUFO-COGNATUS ANOLIS-CAROLINENSIS CROTALUS-ATROX SKIN PROLIFERATION
AN: 198580039312
UD: 1985


TI: Effects of meal size, meal type, body temperature, and body size on the specific dynamic action of the marine toad, Bufo marinus.
AU: Secor-Stephen-M {a}; Faulkner-Angela-C
AD: {a} Department of Biological Sciences, University of Alabama, Box 870344, Tuscaloosa, AL, 35487-0344, USA; E-Mail: ssecor@biology.as.ua.edu, USA
SO: Physiological-and-Biochemical-Zoology. [print] November-December 2002 2002; 75 (6): 557-571.
PY: 2002
DT: Article-
IS: 1522-2152
LA: English
AB: Specific dynamic action (SDA), the accumulated energy expended on all physiological processes associated with meal digestion, is strongly influenced by features of both the meal and the organism. We assessed the effects of meal size, meal type, body temperature, and body size on the postprandial metabolic response and calculated SDA of the marine toad, Bufo marinus. Peak postprandial rates of O2 consumption (VO2) and CO2 production (VCO2) and SDA increased with meal size (5%-20% of body mass). Postprandial metabolism was impacted by meal type; the digestion of hard-bodied superworms (Zophobas larva) and crickets was more costly than the digestion of soft-bodied earthworms and juvenile rats. An increase in body temperature (from 20degree to 35degreeC) altered the postprandial metabolic profile, decreasing its duration and increasing its magnitude, but did not effect SDA, with the cost of meal digestion remaining constant across body temperatures. Allometric mass exponents were 0.69 for standard metabolic rate, 0.85 for peak postprandial VO2, and 1.02 for SDA; therefore, the factorial scope of peak postprandial VO2 increased with body mass. The mass of nutritive organs (stomach, liver, intestines, and kidneys) accounted for 38% and 20% of the variation in peak postprandial VO2 and SDA, respectively. Toads forced to exercise experienced 25-fold increases in VO2, much greater than the 5.5-fold increase experience during digestion. Controlling for meal size, meal type, and body temperature, the specific dynamic responses of B. marinus are similar to those of the congeneric Bufo alvarius, Bufo boreas, Bufo terrestris, and Bufo woodhouseii.
AI: Y
MC: Ingestion-and-Assimilation; Physiology-
ST: Coleoptera-: Insecta-, Arthropoda-, Invertebrata-, Animalia-; Salientia-: Amphibia-, Vertebrata-, Chordata-, Animalia-
OR: Bufo-alvarius (Salientia-); Bufo-boreas (Salientia-); Bufo-marinus [marine-toad] (Salientia-); Bufo-terrestris (Salientia-); Bufo-woodhouseii (Salientia-); Zophobas- [superworm-] (Coleoptera-): food-, larva-
TN: Amphibians-; Animals-; Arthropods-; Chordates-; Insects-; Invertebrates-; Nonhuman-Vertebrates; Vertebrates-
PS: intestine-: digestive-system; kidney-: excretory-system; liver-: digestive-system; stomach-: digestive-system
CB: carbon-dioxide: production-; oxygen-: consumption-
RN: 124-38-9: CARBON DIOXIDE; 7782-44-7: OXYGEN
MI: body-size; body-temperature; meal-size; meal-type; physical-exercise; postprandial-metabolic-response; specific-dynamic-action [SDA-]; standard-metabolic-rate
AN: 200300243711
UD: 20030519

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Search History: bufotenine (76 records)

Record 1 of 76 in BIOSIS Previews 2001/04-2001/05: 14-21

TI:  The chemistry of indoles. CIII. Simple syntheses of serotonin, N-methylserotonin, bufotenine, 5-methoxy-N-methyltryptamine, bufobutanoic acid, N-(indol-3-yl)methyl-5-methoxy-N-methyltryptamine, and lespedamine based on 1-hydroxyindole chemistry.
AU:  Somei-Masanori {a}; Yamada-Fumio; Kurauchi-Takashi; Nagahama-Yoshiyuki; Hasegawa-Masakazu; Yamada-Koji; Teranishi-Sakiko; Sato-Haruhiko; Kaneko-Chikara
SO:  Chemical-and-Pharmaceutical-Bulletin-Tokyo. [print] January, 2001; 49 (1): 87-96.
PY:  2001
LA:  English
AB:  Application of regioselective nucleophilic substitution reactions of 1-hydroxytryptamines to novel and simple syntheses of serotonin (1a), N-methylserotonin (1b), bufotenine (1c), 5-methoxy-N-methyltryptamine (2a), bufobutanoic acid (3a), N-(indol-3-yl)methyl-5-methoxy-N-methyltryptamine (4), and lespedamine (5) are described. Effective syntheses of 5-benzyloxytryptamine and 1-methoxy-2-oxindoles are also reported.
AN:  200100173936
UD:  20010403


Record 2 of 76 in BIOSIS Previews 2000/11-2000/12: 44-52

TI:  Bufotenine: Toward an understanding of possible psychoactive mechanisms.
AU:  McBride-Michael-C {a}
SO:  Journal-of-Psychoactive-Drugs. [print] July-September, 2000; 32 (3): 321-331.
PY:  2000
LA:  English
AB:  A review of the neuropharmacology of the alleged hallucinogen bufotenine is presented, including recent experimental results showing activity similar to LSD and other known hallucinogens (psilocin and 5-MeO-DMT) at the purported hallucinogenic serotonin (5-HT) receptors, 5-HT2A and 5-HT2C. In addition, current reports of computer modeling of the receptors and ligand binding sites give evidence of bufotenine's ability to bind and activate these receptors. While binding and activation of the purported hallucinogenic receptors are not the full extent of the hallucinogenic signature, this evidence shows support for the rationale that the reported lack of the drug's classic hallucinogenic response in human experiments is due to poor ability to cross the blood brain barrier (BBB), not lack of activation of the appropriate brain receptors. Further evidence is reviewed that in some physiological states, some drugs with characteristics similar to bufotenine which do not normally cross the BBB, cross it and enter the brain. While direct human experimental evidence of bufotenine's hallucinogenic activity seems lacking, the above combined factors are considered, and possible explanations of bufotenine's reported psychoactivity are suggested. Additionally, updated experimental models testing the possible nature of bufotenine's hallucinogenic potential are proposed.
AN:  200000520043
UD:  20001122


Record 3 of 76 in BIOSIS Previews 2000/04-2000/06: 14-26

TI:  Development of immunoassays for tyramine and tryptamine toxins of Phalaris aquatica L.
AU:  Skerritt-John-H {a}; Guihot-Simone-L; McDonald-Scott-E; Culvenor-Richard-A
SO:  Journal-of-Agricultural-and-Food-Chemistry. Jan., 2000; 48 (1): 27-32.
FTXT:  EBSCO Online http://www.ebsco.com/online/direct.asp?ArticleID=ARTQ7J5EJC7YVV4YDB05
PY:  2000
LA:  English
AB:  The leaves of the perennial pasture grass Phalaris aquatica L. (phalaris) contain two groups of known toxins, indole alkaloids, primarily dimethyltryptamines and N-methyltyramines, which cause illnesses in grazing animals, especially sheep. Using amino-reactive and phenolic hydroxyl-reactive homobifunctional reagents, simple methods were devised for coupling toxins representative of those in phalaris to carrier proteins and enzymes for ELISA development. ELISAs were produced for both groups of toxins. Dimethyltryptamines were most sensitively detected (lower limit of detection (LLD) of 1 mug/L for bufotenine) using rabbit anti-bufotenine antibodies, coupled to ovalbumin using divinyl sulfone, with detection using a peroxidase conjugate prepared using the same hapten coupled with 1,4-butanediol diglycidyl ether. The assay cross-reacted with other toxins of the same class (N,N-dimethyltryptamine and N,N-dimethyl-5-methoxytryptamine) but not with the structurally related amino acids histidine and tryptophan. The most sensitive N-methyltyramine assay (LLD of 1 mug/mL for N-methyltyramine) utilized antisera to tyramine with N-methyltyramine coupled to peroxidase. Significant cross-reaction was seen with the low-grade toxin hordenine, but detection of tyramine was poorer, whereas the amino acid tyrosine was not detected. These assays could be applied to the analysis of simple extracts of Phalaris leaves with minimal interference. A good correspondence was observed between toxin levels by ELISA and estimates from a more tedious thin-layer chromatography method. The method has now been incorporated in a Phalaris breeding program.
AN:  200000164201
UD:  20000418


Record 4 of 76 in BIOSIS Previews 2000/04-2000/06: 14-26

TI:  Determination of antimigraine compounds rizatriptan, zolmitriptan, naratriptan and sumatriptan in human serum by liquid chromatography/electrospray tandem mass spectrometry.
AU:  Vishwanathan-Karthick; Bartlett-Michael-G; Stewart-James-T {a}
SO:  Rapid-Communications-in-Mass-Spectrometry. 2000; 14 (3): 168-172.
PY:  2000
LA:  English
AB:  Development of a rapid, sensitive and selective method for the determination of antimigraine drugs from human serum is essential for understanding the pharmacokinetics of these drugs when administered concurrently. Solid phase extraction (SPE) using Oasis HLB was used to extract the drugs (sumatriptan, naratriptan, zolmitriptan and rizatriptan) and the internal standard bufotenine from serum. A method based on liquid chromatography/tandem mass spectrometry (LC/MS/MS) was developed and validated to simultaneously quantitate these antimigraine drugs from human serum. The precursor and major product ions of the analytes were monitored on a triple quadrupole mass spectrometer with positive ion electrospray ionization (ESI) in the multiple reaction monitoring (MRM) mode. The base peak in all the analytes is formed by alpha cleavage associated with protonation of the secondary amine. Mechanisms for the formation of the collision-induced dissociation products of these antimigraine compounds are proposed. Linear calibration curves were generated from 1-100 ng/mL with all coefficients of determination greater than 0.99. The inter- and intraday precision (%RSD) were less than 9.3% and accuracy (%error) was less than 9.8% for all components. The limits of detection (LOD) for the method were 250 pg/mL for sumatriptan and 100 pg/mL for the remaining analytes based on a signal-to-noise ratio of 3.
AN:  200000132716
UD:  20000404


Record 5 of 76 in BIOSIS Previews 2000/01-2000/03: 1-13

TI:  Anti-bufotenine monoclonal antibodies and bufotenine immunoreactivities in the brain of the toad, Bufo bufo japonicus.
AU:  Takeda-N {a}
SO:  Society-for-Neuroscience-Abstracts. 1999; 25 (1-2): 177.
PY:  1999
MT:  29th Annual Meeting of the Society for Neuroscience, Part 1, Miami Beach, Florida, USA, October 23-28, 1999
LA:  English
AN:  200000079318
UD:  20000215


Record 6 of 76 in Biosis Previews 1999/01-1999/06

TI:  Conversion of brain serotonin to bufotenine by lung extracts in model animals for psychiatric disorders.
AU:  Takeda-N {a}
SO:  Society-for-Neuroscience-Abstracts. 1998; 24 (1-2) 1104.
PY:  1998
MT:  28th Annual Meeting of the Society for Neuroscience, Part 1, Los Angeles, California, USA, November 7-12, 1998
LA:  English
AN:  199900056875
UD:  19990208

Record 7 of 76 in Biosis Previews 1998/07-1998/12

TI:  Chemical and pharmacological study of higher fungi. II. Comparative investigation of caprophores of some Nematoloma species: Chemical composition and cultural characteristics.
AU:  Badalyan-S-M {a}; Doko-L; Rapior-S; Jacob-M; Andary-C; Mnatsakanyan-B-A; Arutyunyan-L-S; Garibova-L-V
SO:  Mikologiya-i-Fitopatologiya. 1996; 30 (4) 79-86.
PY:  1996
LA:  Russian; Non-English
AB:  Carpophores of N. fasciculare, N. capnoides and N. sublateritium were screened by thin layer chromatography and qualitative chemical reactions in order to detect polyols, free sugars, amino acids, phenolic acids, glicosides, a kaloides, nitrogen-containing compounds and toxins. Arabitol, tregalose, alanine, valine, serine, glutaminic acid, 4-hydroxybenzoic and vanillic acids as well as choline and cortinarine A were mainly observed in aqueous and methanolic extracts of the studies Nematoloma species. Fungal toxins - amanitin, bufotenine, muscarine, muscimol and orellanine were not observed. Glycosides were detected in methanolic and aqueous extracts from N. fasciculare and N. capnoides. Certain differences in chemical composition of N. fasciculare carpophores from France and Germany have been found. They are concerned with the distinguishable variations in glucose, arabitol, 4-hydroxycinnamic, 3,4-dihydroxyphenilacetic and 3,4-dihydroxybenzoic acids as well as in proline, glutaminic acid and asparagine content. Chemical composition of fruit bodies, micro- and macromorphological characteristics and biotic activity of mycelium demonstrated the phylogenetical closeness of N. fasciculare and N. capnoides.
AN:  199800408331
UD:  19980723

Record 8 of 76 in Biosis Previews 1998/07-1998/12

TI:  Chemical and pharmacological study of higher fungi. I. Chemical composition and pharmacological investigation of carpophores of Cortinarius armillatus (Fr.:Fr.) Fr. (Cortinariaceae).
AU:  Badalyan-S-M {a}; Rapior-S; Doko-L; Le-Quang-J; Jacob-M; Serrano-J-J; Andary-C
SO:  Mikologiya-i-Fitopatologiya. 1996; 30 (3) 37-42.
PY:  1996
LA:  Russian; Non-English
AB:  The fruit bodies of Cortinarius armillatus were investigated for polyols, tree sugars and amino acids, phenolic acids, alkaloids, nitrogen content compounds, glycosides and fungal toxins using thin-layer chromatography and qualitative chemical reactions. Arabitol, mannitol, trehalose, fructose, 4-hydroxybenzoic acid, cholin, alanine, proline, serine, asparagine, glycosides and cortinarin A were detected in aqueous and methanolic extract. from the mushroom. Valine, methionine, glutaminic acid and fungal toxins (alpha-amanitin, orellanine, muscarine, muscimol, bufotenine) were not observed within C. armillatus. The single intraperitoneal doses of the methanolic extract from C. armillatus have not been toxic and no induced effects organic pathology up to 2000 mg/kg two weeks after injection to mice. These chemical studies and acute toxicity investigations supported the non-toxicity of C. armillatus. At the content of some chemical substances (4-hydroxybenzoic acid, cholin, steroid glycosides, cortinarin A) this species may be perspective for a further pharmacological investigations.
AN:  199800401277
UD:  19980723

Record 9 of 76 in Biosis Previews 1998/07-1998/12

TI:  A comparison of N,N-dimethyltryptamine, harmaline, and selected congeners in rats trained with LSD as a discriminative stimulus.
AU:  Helsley-Scott {a}; Fiorella-David; Rabin-Richard-A; Winter-J-C
SO:  Progress-in-Neuro-Psychopharmacology-and-Biological-Psychiatry. May, 1998; 22 (4) 649-663.
FTXT:  ScienceDirect (tm) http://www.sciencedirect.com/science?_ob=GatewayURL&_origin=SilverLinker&_urlversion=4&_method=citationSearch&_volkey=0278%2d5846%2322%23649%234&_version=1&md5=5b36a7c4600e9535c6dacbcb7624bef0 ScienceDirect (China) http://elsevier.lib.tsinghua.edu.cn/science?_ob=GatewayURL&_origin=SilverLinker&_urlversion=4&_method=citationSearch&_volkey=0278%2d5846%2322%23649%234&_version=1&md5=5b36a7c4600e9535c6dacbcb7624bef0 ScienceDirect (Taiwan) http://sdos.ejournal.ascc.net/science?_ob=GatewayURL&_origin=SilverLinker&_urlversion=4&_method=citationSearch&_volkey=0278%2d5846%2322%23649%234&_version=1&md5=5b36a7c4600e9535c6dacbcb7624bef0
PY:  1998
LA:  English
AB:  1. A series of N-substituted tryptamines was trained to discriminate LSD (0.1 mg/kg) from saline. 2. Intermediate levels of substitution were elicited by MDMT (76.4%), DMT (77.9%), and DET (48.7%). 6-F-DET produced 41.3% LSD-appropriate responding at a dose of 6.0 mg/kg but only 4 of 8 subjects completed the test session thus precluding statistical analysis. Bufotenine (25.8%) also failed to substitute. Although none of the tryptamines substituted completely for LSD, the pattern of substitution  is consonant with what is known of their activity in humans. MDMT, DMT, and DET are well established in the literature as hallucinogens but the same cannot be said for 6-F-DET and bufotenine. 3. Of the beta-carbolines tested, none substituted for LSD completely and only harmane elicited intermediate substitution (49.5%). No significant generalization of the LSD stimulus to 6-methoxyharmalan, harmaline, or THBC was observed. Thus, in contrast to the tryptamines, scant ability to substitute for  LSD was observed in the beta-carbolines tested. 4. Taken together, the present data indicate that the representative tryptamines employed in the present study exhibit greater similarity to the LSD stimulus than do representative betacarbolines. The receptor interactions responsible for these differences remain to be determined.
AN:  199800326389
UD:  19980602

Record 10 of 76 in Biosis Previews 1997/07-1997/12

TI:  Model animals for each level of methylation in psychiatric disorders.
AU:  Takeda-N
SO:  Society-for-Neuroscience-Abstracts. 1997; 23 (1-2) 1220.
PY:  1997
MT:  27th Annual Meeting of the Society for Neuroscience, New Orleans, Louisiana, USA, October 25-30, 1997
LA:  English
AN:  199799827104

Record 11 of 76 in Biosis Previews 1997/07-1997/12

TI:  Identification of conserved aromatic residues essential for agonist binding and second messenger production at 5-hydroxytryptamine-2A receptors.
AU:  Roth-B-L {a}; Shoham-M; Choudhary-M-S; Khan-N
SO:  Molecular-Pharmacology. 1997; 52 (2) 259-266.
PY:  1997
LA:  English
AB:  Several models of agonist binding to G protein-coupled 5-hydroxytryptamine (5-HT) (serotonin) receptors have highlighted the potential importance of highly conserved aromatic residues for ligand binding and agonist efficacy. In this study, we tested these models by constructing and characterizing a number of point mutations of conserved and nonconserved aromatic residues using the 5-HT-2A receptor as a model system. Mutations of three highly conserved tryptophans (W200A, W336A, and W367A) proposed to reside near the binding pocket markedly reduced agonist affinity and efficacy at 5-HT-2A receptors. Mutations of two other highly conserved aromatic residues postulated to be near the agonist binding site (F340L and Y370A) also had dramatic effects on agonist binding and efficacy. Point mutations of neighboring conserved phenylalanines (F339L and F365L) had minimal effects on agonist binding, although the F365L mutation diminished agonist efficacy. Finally, mutations of two nonconserved aromatic residues (F125L and F383A) not predicted to be near the binding pocket had no effects on agonist binding, potency, or efficacy. Our results are best explained by models that suggest that helices III, V, VI, and VII can form a unit of interacting helices in which highly conserved aromatic residues are oriented toward the center of the helical aggregate to form an aromatic pocket. In addition, our novel results identify a series of aromatic residues essential for agonist-induced second messenger production. These results demonstrate that highly conserved aromatic residues residing in neighboring helices provide the optimum environment for both agonist binding and activation of 5-HT-2A receptors.
AN:  199799742774

Record 12 of 76 in Biosis Previews 1997/07-1997/12

TI:  Synthesis of 131I derivatives of indolealkylamines for brain mapping.
AU:  Sintas-Jose-A; Vitale-Arturo-A {a}
SO:  Journal-of-Labelled-Compounds-and-Radiopharmaceuticals. 1997; 39 (8) 677-684.
PY:  1997
LA:  English
AB:  The synthesis and spectral properties of new radioiodinated indolealkylamines like 2(131I)-iodo-N,N-dimethyltryptamine, 2-( 131I)-iodo-N-methyltryptamine, 2- (131I)-iodo-5-methoxy- N,N-dimethyltryptamine, 2-(131I)-iodo-5-hydroxy-N,N-dimethyltryptamine (2-( 131I)-iodo- bufotenine), and 2-(131I)-iodo-tryptamine and the known 2-( 131I)-iodo-N-acetyl-5-methoxy-tryptamine (2-( 131I)-iodo-melatonine) are described herein. These were synthesized by a high-yield novel method, and their spectral properties are fully described. These compounds are of biological importance and can be used for brain mapping with SPECT technology.
AN:  199799696943

Record 13 of 76 in Biosis Previews 1997/07-1997/12

TI:  Functional and radioligand binding characterization of rat 5-HT-6 receptor stably expressed in HEK293 cells.
AU:  Boess-F-G; Monsma-F-J-Jr; Carolo-C; Meyer-V; Rudler-A; Zwingelstein-C; Sleight-A-J {a}
SO:  Neuropharmacology-. 1997; 36 (4-5) 713-720.
FTXT:  ScienceDirect (tm) http://www.sciencedirect.com/science?_ob=GatewayURL&_origin=SilverLinker&_urlversion=4&_method=citationSearch&_volkey=0028%2d3908%2336%23713&_version=1&md5=5fa699592ef1d46f149ee2908623a2ed ScienceDirect (China) http://elsevier.lib.tsinghua.edu.cn/science?_ob=GatewayURL&_origin=SilverLinker&_urlversion=4&_method=citationSearch&_volkey=0028%2d3908%2336%23713&_version=1&md5=5fa699592ef1d46f149ee2908623a2ed ScienceDirect (Taiwan) http://sdos.ejournal.ascc.net/science?_ob=GatewayURL&_origin=SilverLinker&_urlversion=4&_method=citationSearch&_volkey=0028%2d3908%2336%23713&_version=1&md5=5fa699592ef1d46f149ee2908623a2ed
PY:  1997
LA:  English
AB:  We have stably expressed the rat 5-HT-6 receptor in HEK293 cells at a density of gt 2 pmol/mg protein, as determined in equilibrium binding studies with (3H)-LSD and (3H)-5-HT and compared the affinity of a range of compounds in competition binding experiments with either (3H)-LSD or (3H)-5-HT as radioligand. A variety of tryptamine derivatives were tested and showed a significantly higher affinity when the 5-HT-6 receptor was labelled with (3H)-5-HT, whereas ergoline compounds and several antagonists had higher affinities when (3H)-LSD was used as radioligand. Subsequently we examined the ability of LSD, 5-HT and a number of tryptamine derivatives to stimulate cAMP accumulation in order to determine their agonist potency and efficacy. We observed the following rank order of potency: LSD gt omega-N-methyl-5-HT apprxeq bufotenine apprxeq 5methoxytryptamine gt 5-HT gt 2-methyl-5-HT apprxeq 5-benzyloxytryptamine apprxeq tryptamine gt 5-carboxamidotryptamine mchgt 5-HTQ. LSD, lisuride, 2-methyl-5-HT, tryptamine and 5-benzyloxytryptamine behaved as partial agonists relative to 5-HT. The rank order of potency of the tryptamine compounds correlated well with their affinities determined in binding assays. In addition, we have tested a number of antagonists in this system (rank order of potency: methiothepin, clozapine, mianserin and ritanserin). This characterization of the pharmacological properties of recombinant 5-HT-6 receptor will facilitate the identification of 5-HT-6 receptor-mediated responses in physiological systems.
AN:  199799662148

Record 14 of 76 in Biosis Previews 1997/07-1997/12

TI:  The metabolism of biogenic monoamines during embryogenesis and metamorphosis in two anuran species.
AU:  Takeda-Naokumi
SO:  General-and-Comparative-Endocrinology. 1997; 106 (3) 361-373.
FTXT:  EBSCO Online http://www.ebsco.com/online/direct.asp?ArticleID=ERF6N0G4EBPPC24N0N1U Academic Press IDEAL (European Mirror) http://www.europe.idealibrary.com/links/doi/10.1006/gcen.1997.6885 Academic Press IDEAL (US Mirror) http://www.idealibrary.com/links/doi/10.1006/gcen.1997.6885
PY:  1997
LA:  English
AB:  This study investigated the pathways to many monoamines and their metabolites in the central nervous system of the frog Rana nigromaculata and the toad Bufo bufo japonicus during embryonic development and metamorphosis. Metabolites were analyzed by three-dimensional HPLC. The two species provided evidence of similar pathways, with slightly different timetables for the development of their monoamine systems. During embryonic development, the main metabolic pathways in entire embryos were tyrosine (TYR) fwdarw (3,4-dihydroxyphenylalanine in Bufo) fwdarw 3-hydroxytyramine fwdarw norepinephrine or epinine (EPIN) fwdarw epinephrine, TYR fwdarw tyramine fwdarw (octopamine in Rana) and TYR fwdarw 3-O-methyldopa for catecholamines, and tryptophan fwdarw kynurenine and 5-hydroxytryptamine (5-HT) fwdarw (5-hydroxyindoleacetic acid and N-methyl-5-hydroxytryptamine (N-MET) in Bufo). The monoamine system in the brain was similar during metamorphosis to that during embryogenesis with a few exceptions. The most striking change was the development of the bufotenine (5-hydroxy-N,N-dimethyltryptamine) pathway from 5-HT via N-MET. EPIN and norepinephrine in Rana and octopamine in both species disappeared during metamorphosis. These results are discussed in relation to the roles of the various pathways in development.
AN:  199799613006

Record 15 of 76 in Biosis Previews 1997/01-1997/06

TI:  High-affinity agonist binding is not sufficient for agonist efficacy at 5-hydroxytryptamine-2A receptors: Evidence in favor of a modified ternary complex model.
AU:  Roth-B-L {a}; Choudhard-M-S; Khan-N; Uluer-A-Z
SO:  Journal-of-Pharmacology-and-Experimental-Therapeutics. 1997; 280 (2) 576-583.
PY:  1997
LA:  English
AB:  In this study, the relationship between high-affinity agonist binding and second messenger production was examined at native and mutant 5-hydroxytryptamine-2A receptors. At native 5-hydroxytryptamine-2A receptors all agonists, with the exception of quipazine, discriminated between high- and low-affinity states of the receptor, as determined by analysis of competition binding assays. There was no correlation between the ability of selected agonists to label the high-affinity agonist state and to augment phosphoinositide hydrolysis. Quipazine, which did not discriminate between the affinity states of the receptor, behaved as a full agonist. Similar results were obtained when a point mutation (F340L) of a highly conserved phenylalanine located in transmembrane domain VI was examined. With the F340L mutant, most of the agonists tested labeled significantly fewer high-affinity sites, compared with the native receptor. There was no significant relationship between high-affinity agonist binding and second messenger production. Bufotenine and 4-iodo-3,5-dimethoxyphenylisopropylamine labeled similar percentages of high-affinity agonist binding sites (22% vs. 26%), but 4-iodo-3,5-dimethoxyphenylisopropylamine behaved as a full agonist, whereas bufotenine was devoid of detectable agonist activity. The inability of selected agonists to activate phosphoinositide hydrolysis was not due solely to lower agonist affinity for the mutant receptor, because the binding affinity of quipazine was unchanged by the F340L mutation but quipazine had no detectable agonist activity at the mutant receptor. Our results demonstrate that the ability of an agonist to promote the high-affinity state of the 5-hydroxytryptamine-2, receptor is not correlated with its ability to augment second messenger production. These results are consistent with recent models of G protein-receptor functioning (e.g., modified ternary complex model) that predict that additional transition states of the receptor-ligand complex are essential for agonist e!
fficacy.
AN:  199799427296

Record 16 of 76 in Biosis Previews 1997/01-1997/06

TI:  Effects of some anxiogenic agents on rat brain monoamine oxidase (MAO) A and B inhibitory (tribulin) activity.
AU:  Bhattacharya-Salil-K {a}; Chakrabarti-Amit {a}; Sandler-Merton; Glover-Vivette
SO:  Indian-Journal-of-Experimental-Biology. 1996; 34 (12) 1190-1193.
PY:  1996
LA:  English
AB:  Anxiogenic agents, yohimbine, pentylenetetrazole(PTZ), quinine, bufotenine, flumazenil and isatin were administered (ip) to rats at doses known to induce anxiety in this species. AR the drugs exhibited anxiogenic response on the elevated plus-maze and induced a parallel increase in endogenous brain monoamine oxidase (MAO) inhibitory (tribulin) activity. The intensity of the drug-induced anxiety was fairly well correlated with the magnitude of increase in the MAO A inhibitory component of tribulin but not so with its MAO B inhibitory component. Thus, in the doses used, the degree of anxiogenic activity was PTZ gt yohimbine gt bufotenine gt quinine gt isatin gt flumazenil, in terms of % entries on the open arms of the maze, whereas the magnitude of endogenous MAO A inhibition was PTZ gt yohimbine gt bufotenine gt quinine gt flumazenil gt isatin. The results indicate that the MAO A inhibitory component of tribulin, rather than its MAO B inhibitory component, may be responsible for the postulated function of tribulin as an endogenous marker of anxiety.
AN:  199799340070

Record 17 of 76 in Biosis Previews 1996/07-1996/12

TI:  Bufo toads and bufotenine: Fact and fiction surrounding an alleged psychedelic.
AU:  Lyttle-Thomas {a}; Goldstein-David; Gartz-Jochen
SO:  Journal-of-Psychoactive-Drugs. 1996; 28 (3) 267-290.
PY:  1996
LA:  English
AN:  199699254428

Record 18 of 76 in Biosis Previews 1996/07-1996/12

TI:  Monoclonal antibodies to bufotenine.
AU:  Takeda-Naokuni
SO:  Society-for-Neuroscience-Abstracts. 1996; 22 (1-3) 604.
PY:  1996
MT:  26th Annual Meeting of the Society for Neuroscience, Washington, D.C., USA, November 16-21, 1996
LA:  English
AN:  199699211069

Record 19 of 76 in Biosis Previews 1996/01-1996/06

TI:  Pharmacology of cloned human 5-HT-1D receptor-mediated functional responses in stably transfected rat C6-glial cell lines: Further evidence differentiating human 5-HT-1D and 5-HT-1B receptors.
AU:  Pauwels-Petrus-J {a}; Palmier-Christiane; Wurch-Thierry; Colpaert-Francis-C
SO:  Naunyn-Schmiedeberg's-Archives-of-Pharmacology. 1996; 353 (2) 144-156.
PY:  1996
LA:  English
AB:  This study was undertaken to investigate the pharmacology of human serotonin (5-HT)-1D receptor sites by measuring two functional cellular responses, inhibition of forskolin-stimulated cAMP formation and promotion of cell growth, using transfected rat C6-glial cell lines and a broad series of 5-HT receptor agonists. Stable and separate transfection of a pcDNA3 or pRcRSV plasmid, each containing a cloned human 5-HT-1D receptor gene, in rat C6-glial cells was confirmed with RT-PCR of 5-HT-1D receptor mRNA and radioligand binding with (3H) 5-carboxamidotryptamine (5-CT) and (3H) sumatriptan. The 5-HT-1D receptor density was 350 and 1050 fmol/mg protein for the C6-glial/pcDNA3/5-HT-1D and C6-glial/pRcRSV/5-HT-1D cell line, and forskolin (100 mu-M)-induced cAMP formation was inhibited by 45 and 78% in the presence of 1 mu-M 5HT, respectively. A comparison of the intrinsic agonist activities for sixteen 5-HT receptor ligands with their corresponding binding affinities for the human 5-HT-1D receptor site showed similar results for both cell lines with the exception of the partial agonist m-trifluoro-phenyl-piperazine (TFMPP). Three classes of compounds were observed: 1) efficacious agonists, such as 5-CT, 5-methoxytryptamine, 5HT, sumatriptan, bufotenine, 5-methoxy-3(1,2,3,6-tetrahydro-4-pyridinyl)1H-indole (RU 24,969), tryptamine and 8hydroxy-2(di-n-propilamino)tetralin (8-OH-DPAT), with agonist potency close to their binding affinity; 2) the partial agonists metergoline, 7-trifluoromethyl-4(4-methyl-1-piperazinyl)-pyrolo-(1,2-a) quinoxaline (CGS 12066B), 1-naphthylpiperazine and 2'-methyl-4-(5-methyl-(1,2,4)oxadiazol3-yl)-biphenyl-4-carboxylic acid (4-methoxy-3-(4-methylpiperazin-1-yl)-phenyl)-amide (GR 127,935) with marked intrinsic agonist activity but at concentrations higher than their binding affinity; and 3) the silent antagonists ritanserin, ketanserin and methiothepin, apparently free of intrinsic agonist activity, with antagonist potency close to their binding affinity. The cAMP data were furthe!
r supported by the observed promotion of cell growth by stimulation of both transfected cell lines with sumatriptan under serum-free conditions; half-maximal stimulation was obtained at 4.4 nM (C6-glial/pcDNA3/5-HT-1D) fully in agreement with its EC-50-value (5.7 nM) for inhibition of cAMP formation. This growth promoting effect was antagonised by 1 mu-M methiothepin and not observed in pcDNA3-plasmid-transfected and non-transfected C6-glial cells. A comparative study with a C6-glial/pcDNA3/5-HT-1B cell line expressing a similar amount of cloned human 5-HT-1B receptors (B-max: 360 fmol/mg protein) showed almost no intrinsic agonist activity for metergoline, 1-naphtylpiperazine and GR 127,935. Together with the 5-HT-1D receptor binding selectivity and antagonist activity of ketanserin and ritanserin, the findings define important pharmacological differences between cloned human 5-HT-1D and 5-HT-1B receptor sites.
AN:  199698695456

Record 20 of 76 in Biosis Previews 1996/01-1996/06

TI:  Bufotenine reconsidered as a diagnostic indicator of psychiatric disorders.
AU:  Takeda-Naokuni {a}; Ikeda-Ryoichi; Ohba-Kimitaka; Kondo-Masanori
SO:  Neuroreport-. 1995; 6 (17) 2378-2380.
PY:  1995
LA:  English
AB:  We have analyzed products of the serotonin-degradative pathway, in which both N-methylserotonin and bufotenine are formed in urine specimens of products with psychiatric disorders by three-dimensional HPLC with electrochemical detection. Bufotenine was detected in urine from all autistic patients with mental retardation and epilepsy (n = 18) and many autistic patients (32/47) with mental retardation. Bufotenine was detected in the urine of 15 of 18 patients with depression. Thirteen of 15 schizophrenic patients were also positive for bufotenine. N-methylserotonin was also detected in some cases of each disorder. Only two of 200 urine specimens from healthy controls were positive for bufotenine. Thus, the presence and levels of bufotenine might be useful and important markers of some psychiatric disorders.
AN:  199698655209

Record 21 of 76 in Biosis Previews 1996/01-1996/06

TI:  Differentiation between partial and silent 5-HT-1Dbeta receptor antagonists using rat C6-glial and Chinese hamster ovary cell lines permanently transfected with a cloned human 5-HT-1Dbeta receptor gene.
AU:  Pauwels-Petrus-J {a}; Colpaert-Francis-C
SO:  Biochemical-Pharmacology. 1995; 50 (10) 1651-1658.
PY:  1995
LA:  English
AB:  Intrinsic activities of serotonin (5-HT) receptor ligands at cloned human 5-HT-1Dbeta receptor sites were determined by measuring cAMP responses in two permanently transfected cell types: rat C6-glial and Chinese hamster ovary (CHO)-K1 cells. Both transfected cell lines expressed a similar 5-HT-1Dbeta receptor density (361 to 448 fmol/mg protein) and displayed a number of similar cAMP responses: marked inhibition of forskolin-stimulated cAMP formation by 5-HT; a similar agonist potency and efficacy with 5-carboxamidotryptamine (5-CT), 5-methoxytryptamine, bufotenine, sumatriptan, 7-trifluoromethyl-4(4-methyl-1-piperazinyl)-pyrolo(1,2-a)quinoxaline (CGS 12066B), 5-methoxy-3(1,2,3,6-tetrahydro-4-pyridinyl)1H-indole (RU 24,969), and tryptamine, their maximal effect being comparable to that of 5-HT; less agonist efficacy with m-trifluoro-phenyl-piperazine (TFMPP) (it inhibited at most 63% of stimulated cAMP formation); and antagonist activity against the 5-CT-mediated agonist response with methiothepin, 2'-methyl-4-(5-methyl-(1,2,4)oxadiazol-3-yl)-biphenyl-4-carboxylic acid (4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl)-amide (GR 127,935), and ritanserin. Metergoline and 1-naphtylpiperazine showed different intrinsic activities. In contrast to their pronounced antagonist activity in the transfected CHO-K1 cell line, the antagonist effect was only partial and absent for metergoline and 1-naphtylpiperazine in the transfected C6-glial cell line, respectively. In conclusion, these cell lines are useful as a tool to measure with high sensitivity differences in intrinsic activities of 5-HT receptor ligands and, therefore, discriminate between silent antagonists (no intrinsic activity) and antagonists with intrinsic activity (i.e. partial agonists), even though this intrinsic activity may be relatively weak.
AN:  199698611893

Record 22 of 76 in Biosis Previews 1995/07-1995/12

TI:  Effects of serotonin reagents on bufotenine levels in the brain of Bufo.
AU:  Takeda-Naokuni
SO:  Society-for-Neuroscience-Abstracts. 1995; 21 (1-3) 1370.
PY:  1995
MT:  25th Annual Meeting of the Society for Neuroscience, San Diego, California, USA, November 11-16, 1995
LA:  English
AN:  199598484531

Record 23 of 76 in Biosis Previews 1995/07-1995/12

TI:  Relative drug efficacy of hallucinogen versus non-hallucinogen agonists is signal transduction pathway dependent.
AU:  Berg-K-A {a}; Maayani-S; Clarke-W-P
SO:  Society-for-Neuroscience-Abstracts. 1995; 21 (1-3) 1365.
PY:  1995
MT:  25th Annual Meeting of the Society for Neuroscience, San Diego, California, USA, November 11-16, 1995
LA:  English
AN:  199598484505

Record 24 of 76 in Biosis Previews 1995/07-1995/12

TI:  Tissue distribution, metabolism and effects of bufotenine administered to rats.
AU:  Fuller-R-W {a}; Snoddy-H-D; Perry-K-W
SO:  Neuropharmacology-. 1995; 34 (7) 799-804.
PY:  1995
LA:  English
AB:  Bufotenine (N,N-dimethyl-5-hydroxytryptamine) is a serotonin analog reported to be hallucinogenic. Bufotenine concentrations were measured by liquid chromatography with electrochemical detection after the s.c. injection of bufotenine (1, 30 or 100 mg/kg) into rats. At 1 hr, bufotenine was high in lung, heart and blood and lower in brain and liver. No N-monomethyl-5-hydroxytryptamine was detected, but 5-hydroxyindoleacetic acid (5HIAA) was increased due to bufotenine metabolism. Bufotenine disappeared nearly completely by 8 hr. Bufotenine concentrations were slightly higher in hypothalamus and brain stem than in striatum or cortex; serotonin was slightly decreased, and 5HIAA was increased in these brain regions. Pargyline reduced concentrations of 5HIAA in blood and tissues after bufotenine injection; LY51641 but not deprenyl mimicked pargyline, suggesting type A not type B monoamine oxidase metabolizes bufotenine. Bufotenine injection increased serum corticosterone concentration, an effect not blocked by metergoline at a dose that blocked a similar increase elicited by quipazine. Although only 2% of the serotonin was found in platelet-poor plasma, more than 99% of the bufotenine was found in platelet-poor plasma, indicating that bufotenine is not stored in platelets. These experiments indicate that bufotenine is rapidly eliminated, in part by type A monoamine oxidase, after its injection into rats and that bufotenine penetrates the blood-brain barrier poorly.
AN:  199598458020

Record 25 of 76 in Biosis Previews 1995/07-1995/12

TI:  Investigation of fungal metabolites and acute toxicity studies from fruit-bodies of Hypholoma species (Strophariaceae).
AU:  Badalyan-S-M; Rapior-S {a}; Le-Quang-J; Doko-L; Jacob-M; Andary-C; Serrano-J-J
SO:  Cryptogamie-Mycologie. 1995; 16 (2) 79-84.
PY:  1995
LA:  English
AB:  The fruit-bodies of Hypholoma fasciculare and H. capnoides were screened by thin-layer chromatography to detect polyols, sugars, phenolic acids, alkaloids and fungal metabolites. Mannitol, trehalose, 4-hydroxybenzoic acid, vanillic acid and choline were mainly observed from both Hypholoma species. The fungal toxins, alpha-amanitin, bufotenine, muscarine, muscimol and orellanine were not detected. Acute toxicity studies and toxicological investigations were carried out in mice given single intraperitoneal doses of suspensions of the methanol extracts from H. fasciculare and H. capnoides. Paralysis of the respiratory centre, severe stomachal ulcers and digestive hemorrhages were revealed with H. fasciculare (LD-50 value: 243.29 mg/kg) while no pathology was observed with H. capnoides.
AN:  199598416121

Record 26 of 76 in Biosis Previews 1995/01-1995/06

TI:  Investigation of primary and secondary metabolites in a chemical study of Cortinarius armillatus (Cortinariaceae, Telamonia).
AU:  Badalyan-S-M; Rapior-S {a}; Doko-L; Le-Quang-J; Jacob-M; Serrano-J-J; Andary-C
SO:  Cryptogamie-Mycologie. 1994; 15 (4) 223-228.
PY:  1994
LA:  English
AB:  The fruit-bodies of Cortinarius armillatus were investigated for polyols, sugars, phenolic acids, alkaloids and fungal toxins using thin-layer chromatography methods. Arabitol, mannitol, trehalose, fructose, 4-hydroxybenzoic acid, choline and cortinarine A were detected from aqueous and methanolic extracts of the mushroom. The fungal toxins, alpha-amanitin, orellanine, muscarine, muscimol and bufotenine were not observed. These chemical investigations and acute toxicity studies in mice supported the non-toxicity of C. armillatus.
AN:  199598193420

Record 27 of 76 in Biosis Previews 1994/07-1994/12

TI:  A single point mutation (Phe-340 fwdarw Leu-340) of a conserved phenylalanine abolishes 4-(125I)iodo-(2,5-dimethoxy)phenylisopropylamine and (3H)mesulergine but not (3H)ketanserin binding to 5-hydroxytryptamine-2 receptors.
AU:  Choudhary-M-S; Craigo-S; Roth-B-L {a}
SO:  Molecular-Pharmacology. 1993; 43 (5) 755-761.
PY:  1993
LA:  English
AB:  The molecular processes by which agonists and antagonists bind to serotonin-2 (5-hydroxytryptamine (5-HT-2)) receptors are currently unknown. Three molecular models have proposed that conserved aromatic residues help to anchor the phenyl ring of 5-HT via stacking or pi-pi-type interactions with the 5-HT-2 receptor. To test these models we made single point mutations (Phe-339 fwdarw Leu-339 and Phe-340 fwdarw Leu-340) of two aromatic residues that are conserved among all guanine nucleotide-binding protein-coupled 5-HT receptors and a single point mutation (Phe-125 fwdarw Leu-125) that exchanges a 5-HT-2 for a 5-HT-1c sequence. (3H) Mesulergine binding was abolished by Phe-340 fwdarw Leu-340 and unchanged with the Phe-339 fwdarw Leu-339 and Phe-125 fwdarw Leu-125 mutations, whereas (3-H)ketanserin binding affinity was diminished by the Phe-339 fwdarw Leu-339 mutation and unchanged by Phe-340 fwdarw Leu-340 and Phe-125 fwdarw Leu-125. We also found that the affinities of three ergot derivatives (mesulergine, methysergide, and lisuride) were decreased by 88-1079-fold with only the Phe-340 fwdarw Leu-340 mutation. We also discovered that 4-(125I)iodo-2,5-(dimethoxy)phenylisopropylamine (DOI) binding was abolished in COS-7 cells expressing 5-HT-2 (Phe-340 fwdarw Leu-340) receptors but maintained in cells expressing the Phe-339 fwdarw Leu-339 and Phe-125 fwdarw Leu-125 mutations. Additionally, the K-i values for several agonists and partial agonists (5-HT, DOI, m-chlorophenylpiperazine, trifluoromethylphenylpiperazine, bufotenine, and MK-212) were greatly diminished (26-14,000-fold decrease) only with the Phe-340 fwdarw Leu-340 receptor mutation. Finally, the Phe-340 fwdarw Leu-340 mutant receptors displayed an attenuated or abolished ability to augment phosphoinositide hydrolysis in COS-7 cells with four separate agonists (5-HT, MK-212, bufotenine, and quipazine). Taken together, these results are consistent with the idea that agonists and certain ergot derivatives anchor to 5-HT-2 receptors, in part, via!
 specific interactions with aromatic residue Phe-340 located in transmembrane region VI.
AN:  199497452483

Record 28 of 76 in Biosis Previews 1994/07-1994/12

TI:  Serotonin-degradative pathways in the toad (Bufo bufo japonicus) brain: Clues to the pharmacological analysis of human psychiatric disorders.
AU:  Takeda-N
SO:  Comparative-Biochemistry-and-Physiology-C-Pharmacology-Toxicology-and-Endocrinology. 1994; 107 (2) 275-281.
PY:  1994
LA:  English
AB:  Bufotenine (BUTN) is a hallucinogen with psychotropic effects. High levels of BUTN and its precursor, N-methylserotonin are shown for the first time to occur and to accumulate mainly in the brain during the degradation of serotonin in the central nervous system of the toad, Bufo bufo japonicus. These compounds are concentrated in the hindbrain, which includes the cerebellum and medulla oblongata. BUTN can also be detected in blood and urine specimens from the toad. In humans, autism is a subtype of schizophrenia that appears to be a functional disease of the brain. BUTN can be detected in urine specimens from infant autistic patients. Analysis by three-dimensional HPLC suggests that the presence and levels of BUTN may be important markers for the diagnosis of autism. It appears, therefore, that some aspects of the central nervous system of Bufo may provide useful pharmacological clues to the etiology of human psychiatric diseases, such as autism, that are known to be linked to the methylation of serotonin.
AN:  199497331494

Record 29 of 76 in Biosis Previews 1994/01-1994/06

TI:  Bufotenine has a parachloroamphetamine-like action on the storage and release of serotonin in rat spinal cord synaptosomes.
AU:  Monroe-Philip-J {a}; Smith-D-L; Williams-G-M; Smith-D-J
SO:  Biogenic-Amines. 1994; 10 (3) 273-284.
PY:  1994
LA:  English
AB:  During a recent evaluation of the abilities of 5HT-3 agents to modulate the release of (3H)-5HT from superfused rat spinal cord synaptosomes, bufotenine was found to be capable of increasing basal neurotransmitter efflux via a mechanism which was sensitive to blockade of the neuronal membrane transport carrier (Williams et al., 1992). The present study was undertaken to further characterize the action of bufotenine on 5HT neuronal function. Bufotenine-evoked release of (3H)-5HT was found to be unaltered by the removal of Ca++ from the superfusion media. In addition, using reserpine pre-treated tissues, it was determined that bufotenine releases 5HT primarily from extravesicular sites. A direct interaction of bufotenine with the neuronal membrane transport carrier is suggested by the ability of bufotenine to interact with sites labelled by (3H)-citalopram (K-i=356 +- 31 nM). A carrier mediated mechanism of release is further suggested by a comparable potency in the drug's ability to promote release (EC-50= 892 +- 60 nM). Bufotenine also weakly inhibited MAO activity. These results demonstrate that bufotenine has an action on 5HT neurons comparable to p-chloroamphetamine.
AN:  199497273538

Record 30 of 76 in Biosis Previews 1994/01-1994/06

TI:  Characterization of the 5-HT-4 receptor mediating tachycardia in piglet isolated right atrium.
AU:  Medhurst-Andrew-D; Kaumann-Alberto-J {a}
SO:  British-Journal-of-Pharmacology. 1993; 110 (3) 1023-1030.
PY:  1993
LA:  English
AB:  1. In order to explore whether 5-HT-4 receptor subtypes exist, we have characterized further the 5-HT-4 receptor that mediates tachycardia in the piglet isolated right atrium. All experiments were carried out in the presence of propranolol (400 nm) and cocaine (6 mu-M). We used tryptamine derivatives, substituted benzamides and benzimidazolone derivatives as pharmacological tools. 2. Tachycardia responses to 5-hydroxytryptamine (5-HT) were mimicked by other tryptamine derivatives with the following order of potency: 5-HT gt 5-methoxytryptamine gt -alpha-methyl-5-HT = bufotenine gt 5-carboxamidotryptamine = tryptamine (after treatment with pargyline) gt 5-methoxy-N,N-dimethyltryptamine gt 2-methyl-5-HT. 3. The substituted benzamides were all partial agonists relative to 5-HT except (-)-zacopride which was a full agonist. The stimulant potency order was renzapride gt cisapride = (-)-zacopride gt metoclopramide gt ( + )-zacopride. 4. The benzimidazolone derivatives had contrasting effects. BIMU 8 (endo-N-(8-methyl-8azabicyclo(3.2.1)oct-3-yl)-2,3-dihydro-(1-methyl(ethyl-2-oxo-1H-benzimidazole-1-carboxamide hydrochloride) was a full agonist relative to 5-HT whilst BIMU 1 (endo-N-(8-methyl-8-azabicyclo(3.2.1)oct-3-yl)2,3-dihydro-3-ethyl-2-oxo-1H-benzimidazole-1-carboxamide hydrochloride) was a partial agonist with low intrinsic activity compared to 5-HT but had similar potency. We estimated a pK-B of 7.9 for BIMU 1 antagonism of 5-HT-induced tachycardia. DAU 6215 (N-endo-8-methyl-8-azabicyclo(3.2.1)-oct-3-yl)-2,3-dihydro-2-oxo-1H-benzimidazole-1-carboxamide, hydrochloride) had no chronotropic activity and was found to be a simple competitive antagonist with a pK-B of 7.1 5. SB 203186 (1-piperidinyl)ethyl 1H-indole 3-carboxylate) was a potent antagonist with a pK-B of 8.3. The affinity of SB 203186 was approximately 20 times higher than that of tropisetron (ICS 205-930; pK-B = 6.9) and DAU 6215 (pK-B = 7.0). GR113808 (((1-(2-(methylsulphonyl amino)ethyl)-4-piperidinyl) methyl 1-methyl-1H-indole-3-carboxyla!
te) and SDZ 205-557 ((2-diethylaminoethyl)2-methoxy-4-amino-5-chloro-benzoate) also antagonized 5-HT-induced tachycardia but not by simple competitive blockade. 6. The sinoatrial 5-HT-4 receptor in the piglet has a pharmacological profile that correlates well with 5-HT-4 receptors characterized in rat oesophagus, guinea-pig ileum and colon, mouse embryonic colliculi neurones and human atrium.
AN:  199497035105

Record 31 of 76 in Biosis Previews 1993/07-1993/12

TI:  Activity of serotonin (5-HT) receptor agonists, partial agonists and antagonists at cloned human 5-HT-1A receptors that are negatively coupled to adenylate cyclase in permanently transfected HeLa cells.
AU:  Pauwels-Petrus-J {a}; Van-Gompel-Paul; Leysen-Josee-E
SO:  Biochemical-Pharmacology. 1993; 45 (2) 375-383.
PY:  1993
LA:  English
AB:  The activity of serotonin (5-HT) receptor agonists, partial agonists and antagonists, and various other neurotransmitter receptor antagonists at human 5-HT-1A receptors that are negatively coupled to adenylate cyclase in permanently transfected HeLa cells was investigated. 5-HT-1A receptor-mediated inhibition of adenylate cyclase was studied by measuring inhibition of cAMP accumulation, induced by forskolin. At 100 mu-M forskolin produced a 100-fold increase in cAMP formation: 5-HT concentration dependently inhibited the cAMP formation; maximal inhibition was attained at 1 mu-M 5-HT and represented 90% of the stimulated cAMP formation. Full inhibition was observed with 5-HT-1A receptor agonists: N,N-dipropyl-8-hydroxy-2-aminotetralin (5-OH-DPAT) and flesinoxan, and non-selective 5-HT receptor agonists: d-lysergic acid diethylamide (d-LSD), RU 24,969, bufotenine, methysergide and tryptamine. The rank order of potency of the compounds for inhibiting the cAMP formation corresponded to the rank order of the binding affinities of the drugs for the 5-HT-1A receptor. Partial inhibition was obtained with submicromolar concentrations of buspirone, spiroxatrine and ipsapirone. A slight inhibition was observed with 1 mu-M 5-HT receptor agonist CP 93129 and 1 mu-M 5-HT receptor antagonists mesulergine and BW-501. No inhibition was found with: the 5-HT receptor agonists quipazine, sumatriptan and 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM); the 5-HT receptor antagonist ICS-205,930; and other neurotransmitter receptor antagonists such as pindolol, CGP20712-A, prazosin, sulpiride and pyrilamine. Spiperone and pindolol fully antagonized the agonist-mediated inhibition of forskolin-stimulated cAMP formation. Partial inhibition of the agonist-mediated inhibition of forskolin-stimulated cAMP formation was apparent with 1 mu-M ocaperidone and 1 mu-M ipsapirone. It can be concluded that HeLa cells, permanently expressing human 5-HT-1A receptors, are a valid cellular system for studying the negative coupling of!
 5-HT-1A receptors to adenylate cyclase and the action of compounds thereupon.
AN:  199395123825

Record 32 of 76 in Biosis Previews 1993/07-1993/12

TI:  Nialamide, an MAO inhibitor, increases urinary excretion of endogenously produced bufotenine in man.
AU:  Karkkainen-Jorma {a}; Raisanen-Martti
SO:  Biological-Psychiatry. 1992; 32 (11) 1042-1048.
PY:  1992
LA:  English
AB:  Nialamide, an MAO inhibitor, was given per os (PO) to a normal man who volunteered in two separate trials (total intake 300 mg and 1000 mg, respectively), and his bufotenin excretion was followed by consecutive urine samples. In both experiments the excretion rose well above the values measured from the same test subject when not taking nialamide (median 0.089 nmol/mmol creatinine, range 0.002-1.78). At its highest, the excretion was 16.5 nmol/mmol creatinine, and the maximum urinary output was 495 nmoles (56 mu-g) in 24 hr. The levels of bufotenin in plasma required for the excretion of the latter amounts are not far from those that produce psychic symptoms in man.
AN:  199395079472

Record 33 of 76 in Biosis Previews 1993/01-1993/06

TI:  The monosynaptic connections between the serotonin-containing LP3 and RPaS neurones in Helix are serotonergic.
AU:  Vehovszky-Agnes {a}; Kemenes-Gyorgy; S-Rozsa-Katalin
SO:  Journal-of-Experimental-Biology. 1992; 173 (0) 109-122.
PY:  1992
LA:  English
AB:  Monosynaptic connections between a giant serotonin-containing neurone and its serotonin-containing followers in the snail were studied in isolated preparations of the central nervous system. The presynaptic cell was the LP3 cell in the left pedal ganglion and the followers were the RPa-s cells in the right parietal ganglion. The light microscopical morphology of the pre- and postsynaptic cells was investigated in whole-mount preparations following intracellular injection with a nickel-lysine complex. Axons from LP3 project towards the cerebral and suboesophageal ganglia or run in peripheral nerves which innervate feeding muscles and the foot. The follower neurones (RPa-s) project into nerves which innervate the heart and other visceral organs. The axons of LP3 and the RPa-s cells run in close proximity in the visceral ganglia. Ionophoretic application of serotonin onto the membrane of the postsynaptic RPa-s neurones mimicked the excitatory effect of the stimulation of the presynaptic LP3. Both the synaptic transmission between LP3 and its followers and the excitatory effect of exogenously applied serotonin on the RPa-s neurones decreased or were blocked in the presence of serotonin or the serotonin antagonists tryptamine, bufotenine, 7-methyltryptamine and MDL 72222-EFO2 in the bath. From this, we conclude that the excitatory neurotransmitter between LP3 and followers is serotonin and not some other neurotransmitter which might coexist with serotonin in LP3. The serotonergic monosynaptic connections between LP3 and its right parietal followers may play a role in a variety of serotonin-mediated physiological and behavioural responses forming a link between feeding, locomotion and visceral functions.
AN:  199395074911

Record 34 of 76 in BIOSIS Previews Part 2 (1992)

TI:  5-HT-3 receptors are not involved in the modulation of the potassium-evoked release of (tritiated)-5-HT from spinal cord synaptosomes of rat.
AU:  Williams-G-M; Smith-D-L; Smith-D-J
CS:  Dep. Pharmacol/Toxicol., HSN, West Va. Univ., Morgantown, W. Va. 26506
SO:  Neuropharmacology 31(8): 725-733
PY:  1992
LA:  English
AB:  The ability of 5-HT-3 receptor agonists to modulate the resting efflux or K+-evoked release of (3H) 5-HT from superfused synaptosomes from the spinal cord of the rat was investigated. Phenyl-biguanide did not alter the resting efflux of (3H)5-HIAA or (3H)5-HT or modify the K+-evoked release of (3H)5-HT. 2-Methyl-5-HT (10 mu-M) caused an increase in resting efflux of (3H)5-HIAA, an effect that was blocked by the inhibitor of the uptake of 5-HT fluoxetine. No effect on K+-evoked release of tritium was observed. Bufotenine (100-1000 nM) increased the resting efflux of (3H)5-HT and (3H)5-HIAA. These effects were not antagonized by the 5-HT-3 antagonist ICS 205-930 but were antagonized by fluoxetine. The drug ICS 205-930 (1 mu-M) did not alter resting efflux or block the ability of serotonin (30 and 100 nM) to decrease K+-evoked release of tritium. Quipazine, a potent antagonist of peripheral 5-HT-3 receptors (subnanomolar concentrations), was also unable to alter resting or K+-evoked release of (3H)5-HT. It did, however, attenuate the inhibitory effect 5-HT on K+-evoked release. The concentrations required were in the micromolar range, consistent with the ability of the drug to antagonize the 5-HT-1B autoreceptor. These results support the idea that 5-HT-3 receptors do not act as nerve terminal autoreceptors in the spinal cord of the rat.
AN:  094099266
UD:  199200

Record 35 of 76 in BIOSIS Previews Part 1 (1992)

TI:  Utilization of o-phthalaldehyde-sulphuric acid as a spray reagent in thin-layer chromatographic detection of some indolealkylamines and application to cutaneous secretion extracts of toad species.
AU:  Lima-C-G-D; Pastore-T-C-M; Schwartz-C-A; Cruz-J-S; Sebben-A
CS:  Departamento de Quimica, Universidade de Brasilia, Brasilia, DF 70910, Brazil
SO:  Talanta 38(11): 1303-1308
PY:  1991
LA:  English
AB:  An expansion of the utilisation of o-phthalaldehyde in sulphuric acid medium as spray reagent was carried out when tryptophan and some tryptophan-derived indole alkylamines such as tryptamine, serotonin, bufotenine, dehydrobufotenine and bufotenidine were examined by thin-layer chromatography. Rf-values and limits of detection ranging from 20 (serotonin) to 100 (dehydrobufotenine) ng per spot were found. Application of this reagent for the detection of some of these compounds was carried out, using either methanolic extracts or column chromatographic fractions of the skin secretion of the toads Bufo ictericus and Odontophrymus cultripes.
AN:  093060587
UD:  199200

Record 36 of 76 in BIOSIS Previews Part 1 (1992)

TI:  Actions of bufotenine on the storage and release of serotonin (5HT) from rat spinal cord synaptosomes.
AU:  Monroe-P-J; Smith-D-L; Williams-G-M; Smith-D-J
CS:  Dep. Anesthesiol., West Va. Univ. Health Sci. Cent., Morgantown, W.Va. 26506
SO:  Society for Neuroscience Abstracts 17(1-2): 1176
MT:  21st Annual Meeting of the Society for Neuroscience, New Orleans, Louisiana, USA, November 10-15, 1991. SOC NEUROSCI ABSTR
PY:  1991
LA:  English
AN:  042116483
UD:  199200

Record 37 of 76 in BIOSIS Previews Part 2 (1991)

TI:  Multi-component system of oviposition stimulants for a Rutaceae-feeding swallowtail butterfly, Papilio xuthus (Lepidoptera: Papilionidae).
AU:  Ohsugi-T; Nishida-R; Fukami-H
CS:  Pesticide Res. Inst., Fac. Agric., Kyoto Univ., Kyoto 606, Japan
SO:  Applied Entomology and Zoology 26(1): 29-40
PY:  1991
LA:  English
AB:  Oviposition behavior by females of a Rutaceae-feeding swallowtail butterfly, Papilio xuthus, was stimulated by contact with methanolic extracts of the leaves of Citrus unshiu. The stimulant compounds, active as a complex mixture, were characterized as vicenin-2, narirutin, hesperidin, rutin, adenosine, 5-hydroxy-N-omega-methyltryptamine, bufotenine, (-)-synephrine, (+)-chiro-inositol and (-)-stachydrine. These 10 components, mixed in the proportions found in the host-plant leaves, were shown to account for the activity of C. unshiu extracts to P. xuthus females.
AN:  092017515
UD:  199100

Record 38 of 76 in BIOSIS Previews Part 2 (1991)

TI:  Kinetic characterization of 5-hydroxytryptamine receptor desensitization in isolated guinea-pig trachea and rabbit aorta.
AU:  Ben-Harari-R-R; Dalton-B-A; Osman-R; Maayani-S
CS:  Dep. Anesthesiol., Box 1010, Mount Sinai Med. Cent., New York, N.Y. 10029
SO:  Journal of Pharmacology and Experimental Therapeutics 257(1): 416-424
PY:  1991
LA:  English
AB:  Desensitization of the contractile response mediated by the 5-hydroxytryptamine-2 (5-HT-2) receptor in the isolated guinea-pig trachea and rabbit aorta is a time-dependent process and therefore it has been characterized by an apparent rate constant obtained from a kinetic analysis. Under similar conditions, desensitization of the response in the trachea is 7-fold faster than in the aorta. Desensitization is homologous and reversible and is not affected by inhibition of neuronal and extraneuronal uptake, monoamine oxidase activity, alpha-1 adrenergic, cholinergic muscarinic or histamine H-1 receptors. Desensitization does not depend on removal of epithelium from the trachea or endothelium and adventitia from the aorta or on the release of a stable relaxant factor. It is also not affected by the removal of extracellular Ca++, which is needed for tonic contraction. The dependence of desensitization on agonist concentration, number of receptors and the intrinsic activity of the agonist was determined. The observed values of the rate constants for desensitization and of the peak tension (T peak) in trachea show a saturable dependence on the concentration of 5-HT, indicating that occupancy of the 5-HT-2 receptor is needed for desensitization. The less efficacious agonists, N-methyl serotonin, dimethyltryptamine, quipazine, 5-methoxytryptamine, 5-methyltryptamine, 5-methoxy dimethyltryptamine, 4-hydroxytryptamine and bufotenine induce significantly slower desensitization than 5-HT. A 25 to 75% reduction in 5-HT-2 receptor number by alkylation had no effect on the observed rate constants for desensitization. This work demonstrates that desensitization of the 5-HT-2 receptor is a time- and tissue-dependent process that depends on the occupancy of the receptor but does not depend on the number of receptors. Desensitization depends on intrinsic activity but a quantitative relationship between the observed rate constant for desensitization and intrinsic activity could not be clearly demonstrated.
AN:  092008872
UD:  199100

Record 39 of 76 in BIOSIS Previews Part 1 (1991)

TI:  A peripheral 5-HT-1D-like receptor involved in serotonergic induced hindlimb scratching in rats.
AU:  Berendsen-H-H-G; Broekkamp-C-L-E
CS:  Dep. CNS Pharmacol., Organon International B.V., P.O. Box 20, 5340 BH Oss, Netherlands
SO:  European Journal of Pharmacology 194(2-3): 201-208
PY:  1991
LA:  English
AB:  The pharmacological characteristics of hindlimb scratching induced by serotonergic compounds were studied. We conclude that hindlimb scratching induced by sertonergic compounds is mediated by a serotonin-1D (5-HT-1D) or 5-HT-1D-like receptor outside the blood-brain barrier because hindlimb scratching could be induced by s.c. injection of 5-methoxytryptamine (5-MeOT), 5-carboxyamidotryptamine (5-CT), bufotenine, 5-hydroxytryptamine (5-HT) and tryptamine. These compounds have high affinity for 5-HT-1A and 5-HT-1D receptors. The 5-HT-1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), the 5-HT-1C receptor agonist MK 212, and the mixed 5-HT-1C/5-HT-2 receptor agonists (dl)-1-(2,5 dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and quipazine did not induce hindlimb scratching. Rather, the latter compounds attenuated 5-MeOT-induced hindlimb scratching. The 5-HT releasing compounds fenfluramine and p-chloroamphetamine (PCA) inhibited whereas the 5-HT re-uptake inhibitors fluvoxamine and indalpine potentiated 5-MeOT-induced hindlimb scratching. 5-MeOT-induced hindlimb scratching could be inhibited dose dependently by the alpha-2-adrenoceptor blockers yohimbine and rauwolsince, which also have high affinity for 5-HT-1D receptors, whereas the alpha-2-adrenoceptor blocker piperoxan only weakly counteracted hindlimb scratching. Haloperidol, apomorphine, clonidine and methiothepin strongly attenuated hindlimb scratching, atropine, naloxone and ICS 205930 attenuated it weakly whereas domperidone, methylatropine and mepyramine were inactive in doses up to 10 mg/kg. Hindlimb scratching induced by 5-MeOT was potentiated by the 5-HT receptor antagonists metergoline, methylsergide, mesulergine, mianserin, ritanserin and xylamidine. Hindlimb scratching was not induced by i.c.v. injection of 5-MeOT. This lack of i.c.v. activity of 5-MeOT and the effect of xylamidine suggests that the site of action for induction of hindlimb scratching outside the blood-brain barrier.
AN:  091123936
UD:  199100

Record 40 of 76 in BIOSIS Previews Part 1 (1991)

TI:  A new 5-hydroxyindole derivative with preferential affinity for 5-HT-1B binding sites.
AU:  Boulenguez-P; Chauveau-J; Segu-L; Morel-A; Lanoir-J; Delaage-M
CS:  CNRS, Laboratoire Neurobiologie, E6 B.P. 71, 31 Rue Joseph Aiguier, 13402 Marseille Cedex 09, Fr
SO:  European Journal of Pharmacology 194(1): 91-98
PY:  1991
LA:  English
AB:  The affinites of several 5-hydroxy-indole derivatives for serotonin-1 (5-HT-1) binding site subtypes, labeled with 2 nM (3H)5-HT, were assessed by quantitative autoradiography on rat brain sections. The results obtained with known ligands, namely 5-hydroxytryptamine (5-HT), 5-methoxytryptamine (5-Me-OT), 5-methoxy-N,N-dimethyl-tryptamine (5-Me-ODMT), 5-hydroxy-N,N-dimethyl-tryptamine (bufotenine) and 8-hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT) demonstrate the reliability and the advantages of this technique for pharmacological studies. Novel serotonin derivatives were synthesized by carboxymethylation of the hydroxyl group. One of those new ligands, serotonin-O-carboxy-methyl-glycyl-tyrosinamide (S-CM-GTNH-2), inhibited 2 nM (3H)5-HT binding to the substantia nigra with an IC-50 of 22.4 nM, a value which is 22 times lower than that found in the dentate gyrus and choroid plexus. This demonstrates the preferential affinity of S-CM-GTNH-2 for 5-HT-1B versus 5-HT-1A and 5-HT-1C binding sites. S-CM-GTNH-2 contains a tyrosine residue, which may be useful for the synthesis of a radioactive iodinated molecule and for the preparation of 'long-lasting lignands' linked through peptide bonds with a protein. These derivatives could be of great interest for ultrastructural and behavioral studies relevant to 5-HT-1B sites.
AN:  091122783
UD:  199100

Record 41 of 76 in BIOSIS Previews Part 1 (1991)

TI:  Effect of 5HT-3 agonists on in vitro tritium-5HT efflux.
AU:  Williams-G-M; Smith-D-L; Smith-J
CS:  Dep. Physiol., WVU-HSN, Morgantown, W.V. 26506
SO:  Society for Neuroscience Abstracts 16(2): 1300
MT:  20th Annual Meeting of the Society for Neuroscience, St. Louis, Missouri, USA, October 28-November 2, 1990. SOC NEUROSCI ABSTR
PY:  1990
LA:  English
AN:  040090156
UD:  199100

Record 42 of 76 in BIOSIS Previews Part 2 (1990)

TI:  Bufotenine: Actions of 5-HT-3 receptors.
AU:  Cramer-W; Van-Drimmelen-M; Long-S; Tulp-M
CS:  Dep. Pharmacol., Duphar B.V., P.O. Box 900 1380 DA Weesp, Netherlands
SO:  European Journal of Pharmacology 183(6): 2148-2149
MT:  XIth International Congress of Pharmacology, Amsterdam, Netherlands, July 1-6, 1990. EUR J PHARMACOL
PY:  1990
LA:  English
AN:  039112372
UD:  199000

Record 43 of 76 in BIOSIS Previews Part 2 (1990)

TI:  Possible involvement of 5HT-1D receptors in drug induced hindlimb scratching in rats.
AU:  Berendsen-H-H-G; Broekkamp-C-L-E; Van-Delft-A-M-L
CS:  Dep. CNS Pharmacology, Organon International B.V., P.O. Box 20, 5340 BH, Oss, Neth
SO:  European Journal of Pharmacology 183(5): 1924-1925
MT:  XIth International Congress of Pharmacology, Amsterdam, Netherlands, July 1-6, 1990. EUR J PHARMACOL
PY:  1990
LA:  English
AN:  039112114
UD:  199000

Record 44 of 76 in BIOSIS Previews Part 1 (1990)

TI:  Differential interactions of indolealkylamines with 5-hydroxytryptamine receptor subtypes.
AU:  McKenna-D-J; Repke-D-B; Lo-L; Peroutka-S-J
CS:  Dep. Neurol., Stanford Univ. School Med., Stanford, Calif. 94305, USA
SO:  Neuropharmacology 29(3): 193-198
PY:  1990
LA:  English
AB:  Affinities of drugs for 21 indolealkylamine derivatives, some with putative hallucinogenic activity, were determined at 5-HT-1A, 5-HT-2A and 5-HT-2B recognition sites, using radioligand competition studies. Nearly all of the derivatives displayed greatest potency for the 5-HT-2A receptor, labelled by (125I)R-(-)DOI in the cortex of the rat. MOst derivatives displayed 2-10 times lower affinity at the HT-2B receptor labelled by (3H)ketanserin in bovine cortex. Derivatives lacking ring substituents displayed lower affinities for all of the recognition sites, compared to derivatives substituted in the 4- or 5-position of the indole ring. The 4-hydroxylated derivatives displayed 25-380-fold selectivity for the 5-HT-2A site, vs the 5-HT-1A site, while the 5-substituted derivatives displayed approximately equal potency at the 5-HT-1A and 5-HT-2A sites. Affinity of all the compounds at the 5-HT-2B site was greater than 300 nM. The 6-substitued derivatives displayed greater than micromolar affinities for all of the 5-HT recognition sites examined. The size of the N,N-dialkyl substituent was a secondary determinant of affinity, with groups larger than N,N-diisopropyl resulting in a marked reduction in affinity at both the 5-HT-2A and 5-HT-1A recognition sites. This study demonstrated that hallucinogenic 4-hydroxy-indolealkylamines, like psychotomimetic phenylisopropylamines, bind potently and selectively to the 5-HT-2A recognition site, labelled by (125I)R-(-)DOI. This provides further evidence indicating that this recently described subtype of the 5-HT-2 receptor may partially mediate the action of hallucinogenic agents.
AN:  089130085
UD:  199000

Record 45 of 76 in BIOSIS Previews Part 1 (1990)

TI:  5-Hydroxytryptamine (5-HT)-induced endothelium-dependent relaxation of pig coronary arteries is mediated by 5-HT receptors similar to the 5-HT-1D receptor subtype.
AU:  Schoeffter-P; Hoyer-D
CS:  Preclinical Res., 386/527, Sandoz Ltd., Ch-4002 Basel, Switzerland
SO:  Journal of Pharmacology and Experimental Therapeutics 252(1): 387-395
PY:  1990
LA:  English
AB:  The 5-hydroxytryptamine (5-HT) receptor mediating endothelium-dependent relaxation of pig coronary arteries was characterized using a variety of 5-HT receptor agonists and antagonists. Unrubbed (with endothelium preserved) rings precontracted by prostaglandin F-2alpha in the presence of ketanserin relaxed in an endothelium-dependent manner to 5-HT, 5-carboxamidotryptamine and 5-methoxytryptamine with about equal potency and efficacy. By comparison, bufotenine, 3-(dimethylamino)ethyl-N-methyl-1H-indole-5-methane sulfonamide, (-)-alpha-methyl-5-HT, N,N-dipropyl-5-carboxamidotryptamine and 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H indole were half-efficient and other drugs (in particular the 5-HT-1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin) were inactive as agonists up to 0.1 mM. The effect of 5-carboxamidotryptamine was antagonized in an apparently competitive manner by 15 drugs. Among the most potent antagonists (mean pK-B value) were the nonselective 5-HT receptor antagonists, methiothepin (7.30) and metergoline (6.86), the 5-HT-1A/5-HT-1D receptor ligand, 1-(2-(4-amino-phenyl)ethyl)-4-(3-trifluoromethylphenyl)-piperazine (7.02), the 5-HT-1A/5-HT-1B/5-HT-1D receptor ligand, 7-trifluoromethyl-4-(4-methyl-1-piperazinyl)-pyrrolo(1,2,-a)quinoxaline 1 (6.73) and yohimbine (6.37). Selective ligands for 5-HT-1A receptors were either inactive (8-hydroxy-2-(di-n-propylamino)tetralin hydrobromide) or poorly active (spiperone, 4.44). Beta-adrenoceptor antagonists with affinity for 5-HT-1A and 5-HT-1B receptors weakly antagonized the effect of 5-carboxamidotryptamine (pK-B values ltoreq 5.32), as did the 5-HT-1C/5-HT-2 receptor antagonist, mesulergine (5.30) and the yohimbine isomer, corynanthine (4.85). Methysergide was clearly a noncompetitive antagonist. Antagonist pK-B values correlated well (r = 0.81, P = 0.001) and exclusively with pK-D values at the 5-HT-1D binding site. It is concluded that the 5-HT receptor mediating endothelium-dependent relaxation of pig coronary arteries shares !
similarities with the 5-HT-1D receptor subtype.
AN:  089096218
UD:  199000

Record 46 of 76 in BIOSIS Previews Part 2 (1989)

TI:  Hallucinogenic drugs are partial agonists of the human platelet shape change response: A physiological model of the 5-HT-2 receptor.
AU:  McClue-S-J; Brazell-C; Stahl-S-M
CS:  Merck Sharp and Dohme Res. Lab., Neuroscience Res. Centre, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR England
SO:  Biological Psychiatry 26(3): 297-302
PY:  1989
LA:  English
AB:  We have assayed several phenylalkylamine and indolealkylamine hallucinogens, as well as structurally similar nonhallucinogens, for their effect on human platelet shape change, a physiological model for the central serotonergic 5-HT-2 receptor. The hallucinogenic drugs lysergic acid diethylamide (LSD-25), N,N-dimethyltryptamine (N,N-DMT), 5-methoxy-N,N-dimethyltryptamine (5-MeODMT), 4-iodo-2,5-dimethoxyphenylisopropylamine (DOI), bufotenine, and mescaline all showed a characteristic 5-HT-2 partial agonist effect on platelet shape change. Nonhallucinogens with structural similarity to hallucinogens did not share this profile. Lisuride, methysergide, and lysergic acid showed antagonism of 5-HT-induced shape change, but none were shape change agonists. Other "psychoactive" or mood-altering drugs (cocaine, amphetamine, phencylidine) showed poor antagonism of 5-HT-induced platelet shape change. This work refines recent ideas that some of the behavioral effects of LSD-type hallucinogens in humans are due to their actions at 5-HT-2 receptors and suggests that these hallucinogens are partial 5-HT-2 agonists.
AN:  088069076
UD:  198900

Record 47 of 76 in BIOSIS Previews Part 2 (1989)

TI:  5-HT-1C receptor-mediated stimulation of inositol phosphate production in pig choroid plexus: A pharmacological characterization.
AU:  Hoyer-D; Waeber-C; Schoeffter-P; Palacios-J-M; Dravid-A
CS:  Preclinical Res., 386/525, Sandoz Ltd., CH-4002 Basel, Switzerland
SO:  Naunyn-Schmiedeberg's Archives of Pharmacology 339(3): 252-258
PY:  1989
LA:  English
AB:  1) 5-HT (5-hydroxytryptamine, serotonin) induces inositol phosphate production in a pig choroid plexus preparation. This effect has been pharmacologically characterized and the data compared to those obtained from radioligand binding studies performed with (3H)mesulergine to 5-HT-1C sites in pig choroid plexus membranes. 2) The rank order of potency of agonists stimulating inositol phosphate production was: alpha-methyl-5-HT gt 1-methyl-5-HT gt DOI gt bufotenine = SKF 83566 = 5-HT gt 5-MeO-DMT gt 5-MeOT = RU 24969 gt SCH 23390 gt 5-CT. 8-OH-DPAT was virtually devoid of activity at 100 mu-ol/l. 3) The increase in inositol phosphate production induced by 5-HT and other agonists was surmountably antagonised by mesulergine, ketanserin and spiperone with pK-B values of 8.7, 6.7 and 5.3, respectively. 4) The rank order of potency of antagonists was: metergoline gt mesulergine gt LY 53857 gt ritanserin gt methiothepin gt mianserin gt cyproheptadine gt pirenperone gt cinanserin gt ketanserin gt spiperone. The following antagonists were virtually devoid of activity at 100 mu-mol/l; pindolol, 21-009 and yohimbine. 5) The results obtained both with agonists and antagonists strongly support the view that 5-HT 1C receptors mediate agonist induced production of inositol phosphates in pig choroid plexus. This is illustrated by the close similarity between 5-HT-1C binding and stimulation of inositol phospholipid turnover in this preparation. 6) The present data also show that compounds believed to be selective for dopamine D1 receptors (SKF 83566, SCH 23390) or 5-HT-2 receptors (DOI, alpha-methyl-5-HT, LY 53857, ritanserin, cyproheptadine) also interact with 5-HT-1C receptors. 7) A case can be made for the 5-HT-1C receptor, with its similarities to the 5-HT-2 receptor in terms of pharmacology and second messenger coupling, being a 5-HT-2 receptor subtype.
AN:  088018110
UD:  198900

Record 48 of 76 in BIOSIS Previews Part 2 (1989)

TI:  Serotonin involvement during in vitro conditioning of Hermissenda.
AU:  Grover-L-M; Farley-J; Auerbach-S-B
CS:  Dep. Psychol., Indiana Univ., Psychol. Build., Bloomington, Indiana 47405
SO:  Brain Research Bulletin 22(2): 363-372
PY:  1989
LA:  English
AB:  To determine if serotonin may be involved in associative conditioning-produced changes in the excitability and photoresponses of Type B photoreceptors, isolated nervous systems were exposed to an in vitro conditioning procedure (16, 19, 27) in the presence or absence of drugs that alter normal serotonergic neurotransmission. Pairings of light and intracellular depolarization of a caudal hair cell (in vitro conditioning) produced a pairing-specific depolarization of Type B photoreceptors that was accompanied by an increase in resting input resistance. Treatment of nervous systems with pharmacological agents which disrupt 5-HT neurotransmission attenuated membrane potential and input resistance changes of Type B photoreceptors. These drugs included serotonin uptake inhibitors (imipramine, fluoxetine), a receptor antagonist (bufotenine), and a neurotoxin (5,7-dihydroxytryptamine; 5,7-DHT). Yohimbine, an alpha-2-receptor antagonist, was without effect. These results, and those in the accompanying papers (9,22), suggest that serotonin modulates Type B photoreceptor excitability during associative conditioning.
AN:  088005266
UD:  198900

Record 49 of 76 in BIOSIS Previews Part 1 (1989)

TI:  A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system.
AU:  Dumuis-A; Bouhelal-R; Sebben-M; Cory-R; Bockaert-J
CS:  Centre CNRS-INSERM Pharmacologie-Endocrinologi, Rue de la Cardonille, 34094 Montpellier Cedex 2, Fr
SO:  Molecular Pharmacology 34(6): 880-887
PY:  1988
LA:  English
AB:  A nonclassical 5-hydroxytryptamine (5-HT) receptor mediates the stimulation of adenylate cyclase activity in mouse embryo colliculi neurons in primary culture. The pharmacological profile characterized with agonists and antagonists suggests that this 5-HT receptor does not appear to correspond to a known 5-HT receptor. On this 5-HT receptor, 5-HT (EC-50 = 109 +- 17 nM) and 5-methoxytryptamine (5MeOT) were equipotent agonists. The other tryptamine derivatives, 5-carboxamidotryptamine (5-CT) and 5-methoxy-N,N-dimethyltryptamine (5-MeOT-N,N-DMT), were full potent agonists, whereas tryptamine, bufotenine, and 2-CH-3-5-HT were weak partial agonists. Two selective 5-HT-1A agonists: 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) and ipsapirone, could not stimulate adenylate cyclase. RU 24969, a tetrahydropyridoindole derivative that is a potent 5-HT-1A and 5-HT-1B agonist was also inactive, whereas RU 28253, another member of this series, could stimulate cAMP production. The action of antagonists acting on 5-HT-1 or 5-HT-2 receptors, such as methiothepin (5-HT-1 and 5-HT-2), metergoline (5-HT-1 and 5-HT-2), spiperone (5-HT-1A and 5-HT-2), (-)-pindolol (5-HT-1B), mesulergine (5-HT-1C), and ketanserin (5-HT-2), were almost inactive in reversing the 5-HT stimulating effect. The selective 5-HT-3 antagonist ICS 205 930 was a full competitive antagonist at this receptor. Nevertheless, MDL 72222, which is also a 5-HT-3 antagonist, was very weak in antagonizing the 5-HT stimulatory effect. A receptor with similar characteristics has also been found in guinea pig hippocampal membranes. In these membranes, the second receptor of low affinity for 5-HT, termed R-L, which is positively coupled to adenylate cyclase, was also antagonized by ICS 205 930. The relatively low affinity of this hippocampal receptor for 5-CT, its stimulation by RU 28253 but not by RU 24969, and its previously reported pharmacological characteristics support the contention that this 5-HT receptor and the 5-HT receptor of mouse embryo collic!
uli neurons in primary culture (both positively coupled to cAMP formation) present great homologies. Inasmuch as none of the classical specific 5-HT-1 and 5-HT-2 agonists or antagonists interact with these 5-HT receptors, it is unlikely that they belong to 5-HT-1 or 5-HT-2 receptor categories. Furthermore, inasmuch as only one 5-HT-3 antagonist (ICS 205 930) blocks their activity and another 5-HT-3 agonist (MDL 72222), as well as the specific 5-HT-3 agonist 2-CH-3-5-HT, were almost inactive, the possibility that they belong to the 5-HT-3 category is excluded. We propose that the 5-HT receptor of mouse embryo colliculi neurons, as well as the low affinity 5-HT receptor (R-L) of the guinea pig hippocampus, belong to a new category of 5-HT receptors that we suggest calling 5-HT-4.
AN:  087062327
UD:  198900

Record 50 of 76 in BIOSIS Previews Part 2 (1988)

TI:  Urinary excretion of free bufotenine by psychiatric patients.
AU:  Karkkainen-J; Raisanen-M; Naukkarinen-H; Spoov-J; Rimon-R
CS:  Child. Hosp., Univ. Helsinki, SF-00290 Helsinki, Finland
SO:  Biological Psychiatry 24(4): 441-446
PY:  1988
LA:  English
AN:  035058056
UD:  198800

Record 51 of 76 in BIOSIS Previews Part 1 (1988)

TI:  Pharmacology of 5-hydroxytryptamine-1A receptors which inhibit cyclic AMP production in hippocampal and cortical neurons in primary culture.
AU:  DUMUIS-A; SEBBEN-M; BOCKAERT-J
CS:  Cent. CNRS-INSERM Pharmacol.-Endocrinol., Rue Cardonille, 34094 Montpellier, Fr
SO:  MOLECULAR PHARMACOLOGY 33(2): 178-186
PY:  1988
LA:  English
AB:  Serotonin (5-hydroxytryptamine, 5-HT) inhibited the formation of cAMP promoted by vasoactive intestinal polypeptide, plus forskolin, in mouse hippocampal and cortical neurons in primary culture. The rank order of potencies of classical 5-HT-1 agonists in inhibiting cAMP formation in hippocampal neurons was 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) gt 5-carboxamidotryptamine (5-CT) gt d-lysergic acid diethylamide gt 5-HT gt 5-methoxy-N,N-dimethyltryptamine (5-MeO-N,N-DMT) gt RU 24969 gt ipsapirone gt bufotenine gt buspirone (half-maximal efficacy (EC-50) = 7, 18, 30, 52, 90, 102, 100, 110, and 128 nM, respectively). All the tryptamine derivatives substituted in position 5 of the indol were potent agonists (5-HT, 5-CT, 5-MeO-N,N-DMT, 5-methoxytryptamine, and bufotenine), whereas tryptamine, N-methyltryptamine, and N,N-dimethyltryptamine were poor agonists. The most potent antagonists tested were spiperone, (+-)-pindolol, (+-)-cyanopindolol, WB4101, and methiothepin, the affinity of spiperone for this receptor being 22 nM. In contrast, ketanserin, a specific 5-HT-2 antagonist, and 5-HT-3-selective drugs (ICS 205 930 and MDL 72222) were very weak in antagonizing the 5-HT-inhibited cAMP formation. The pharmacological profiles of 5-HT receptors mediating the inhibition of cAMP formation indicate that these receptors correspond to the 5-HT-1A-binding site subtypes. Experiments with the Bordetella pertussis toxin indicate that the 5-HT-1A receptor mediating inhibition of cAMP production involves a pertussis toxin-sensitive GTP-binding protein. In the absence of VIP, cAMP formation could be stimulated through a 5-HT receptor, but the specific 5-HT-1A agonists, 8-OH-DPAT and RU 24969 did not stimulate cAMP production. These results suggest that in mouse embryonic hippocampal neurons, the 5-HT-1A receptors, which are negatively coupled to adenylate cyclase, are distinct from the receptor positively coupled to this enzyme. The pharmacological characterization of the 5-HT receptor negatively coupled to !
adenylate cyclase in mouse embryonic cortical neurons indicates that it differs from the 5-HT-1A receptor found in hippocampal neurons. Its main differences with the 5-HT-1A receptor in hippocampal neurons are as follows: 8-OH-DPAT was only a poor partial agonist in cortical neurons, whereas it was the best full agonist in hippocampal neurons; and metergoline and methysergide as well as the anxiolytic drugs, ipsapirone and buspirone, which were potent agonists in hippocampal neurons, were competitive antagonists in cortical neurons. Since 5-HT receptors inhibiting cAMP formation in embryonic cortical neurons share many other pharmacological characteristics with a typical 5-HT-1A receptor, we can conclude that it is likely to be a nontypical 5-HT-1A receptor.
AN:  085104314
UD:  198800

Record 52 of 76 in BIOSIS Previews Part 2 (1987)

TI:  Skin potions.
AU:  Milstone-L-M
CS:  Dep. Dermatol., Yale Univ. Sch. Med., New Haven, Conn. 06510
SO:  Archives of Dermatology 123(8): 1087-1088
PY:  1987
LA:  English
AN:  033109123
UD:  198700

Record 53 of 76 in BIOSIS Previews Part 2 (1987)

TI:  7-Amino-8-(iodine-125)-ketanserin, a highly sensitive, serotonin S-2 receptor ligand.
AU:  Wouters-W; Van-Dun-J; Laduron-P-M
CS:  Dep. Biochem. Pharmacol., Janssen Pharm., Turnhoutseweg 30, B-2340 Beerse, Belgium
SO:  Biochemical Pharmacology 35(19): 3199-3202
PY:  1986
LA:  English
AN:  032023429
UD:  198700

Record 54 of 76 in BIOSIS Previews Part 1 (1987)

TI:  Chemical and enzymatic oxidative coupling of 5-hydroxy-N,N-dimethyltryptamine with amines.
AU:  BABIN-F; HUYNH-DINH-T
CS:  Inst. Pasteur, Unite de Chimie Organique, Dep. de Biochimie et Genetique Molecular, UA CNRS 487, 75724 Paris Cedex 15, France
SO:  JOURNAL OF MEDICINAL CHEMISTRY 30(7): 1239-1241
PY:  1987
LA:  English
AB:  As part of a program aiming to obtain a covalent labeling of serotoninergic receptors we have studied the oxidative coupling of serotonin derivatives with amino compounds. The oxidation of bufotenine (2) by MnO-2 and human ceruloplasmin followed by the Michael type addition with dansylcadaverine and dansyllysine gave a fluorescent adduct identified as fused oxazole structure 4.
AN:  084059719
UD:  198700

Record 55 of 76 in BIOSIS Previews Part 1 (1987)

TI:  Pharmacological characterization of two 5-hydroxytryptamine receptors coupled to adenylate cyclase in guinea pig hippocampal membranes.
AU:  SHENKER-A; MAAYANI-S; WEINSTEIN-H; GREEN-J-P
CS:  Dep. Pharmacol., Mount Sinai Sch. Med., One Gustave L. Levy Place, New York, NY 10029
SO:  MOLECULAR PHARMACOLOGY 31(4): 357-367
PY:  1987
LA:  English
AB:  Two 5-hydroxytryptamine (5-HT) receptors mediate stimulation of adenylate cyclase activity in membranes of adult guinea pig hippocampus. The two receptors were characterized with agonists and antagonists and with the aid of computerized curve-fitting procedures. Each receptor mediates about 50% of the maximal response to 5-HT. 5-HT is about 10-fold more potent in eliciting response through one cyclase-linked receptor (R-H) than the other (R-L). The concentrations of 5-HT that elicit half-maximal response through R-H and R-L are 43 +- 6 nM and 414 +- 53 nm, respectively. 5-Methoxytryptamine (5-MeOT) and 5-HT are approximately equipotent at each receptor. The agonists tryptamine and bufotenine are less potent than 5-HT at both receptors, and each is about 50-fold selective for R-H. The two receptors are best discriminated by the agonists 5-carboxamidotryptamine (5-CONH-2-T) and 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), both of which are selective for R-H. 5-CONH-2-T is about 7-fold more potent than 5-HT at R-H. The rank order of agonist potencies at R-H (5-CONH-2-T gt 8-OH-DPAT = 5-HT = 5-MeOT gt bufotenine gt tryptamine) differs from that at R-L (5-HT = 5-MeOT gt bufotenine gt tryptamine = 5-CONH-2-T gt 8-OH-DPAT). Spiperone acts as a simple competitive antagonist at R-H, with a dissociation constant of 20 nM, but it is at least 100-fold less potent as an antagonist at R-L. The relatively low affinities of the selective 5-HT antagonists ketanserin and MDL 72222 for R-H and R-L indicate that neither receptor may be classified as the 5-HT-2 or as the 5-HT-3 (i.e., peripheral neuronal) type. The characteristics of R-H suggest that it is a functional correlate of the 5-HT-1A-binding site in brain. R-L appears not to correspond to a known 5-HT-binding site, but it may be homologous to receptors that mediate 5-HT-stimulated adenylate cyclase activity in other systems such as infant rat colliculi. R-H and R-L may also mediate stimulation of adenylate cyclase activity by 5-HT in hippocampal membran!
es of adult rat.
AN:  084038332
UD:  198700

Record 56 of 76 in BIOSIS Previews Part 1 (1987)

TI:  Tryptamine and some related molecules block the accumulation of a light-sensitive pool of cyclic AMP in the dark-adapted, dark-incubated mouse retina.
AU:  COHEN-A-I; BLAZYNSKI-C
CS:  Dep. Ophthalmology, Box 8096, Washington Univ. Sch. Med., 660 South Euclid Ave., St. Louis, MO 63110, USA
SO:  JOURNAL OF NEUROCHEMISTRY 48(3): 729-737
PY:  1987
LA:  English
AB:  Dark-adapted retinas of mice (C57BL/6J) incubated in the dark in media containing 1 mM 3-isobutylmethylxanthine (IBMX) or 5 mM Co-2+ accumulate cyclic AMP (cAMP). A portion of this pool is light sensitive, as light can prevent or reverse its accumulation. Similarly, tryptamine, serotonin, 5-methoxytryptamine, bufotenine, and 5-methoxydimethyltryptamine can block the accumulation of the light sensitive pool of cAMP, whereas tryptophan, melatonin, N-acetylserotonin, 5-methoxytryptophol, and tetrahydro-beta-carbolines are inactive. The phenomenon is not seen with mutant mouse retinas (rd/rd), which lack most photoreceptors, but persists in abnormal retinas containing photoreceptors but with extensive neuronal depletion in the inner retina. Tryptamine also inhibits cAMP accumulation in either dark or light-adapted retinas exposed to forskolin alone but not in media containing high levels of forskolin plus 1 mM IBMX. There is some suggestion that serotonin 5-HT antagonists can partially reverse the action of the tryptamines, but hitherto undescribed receptors may be involved. Current data suggest that photoreceptors are the target for the action of the tryptamines.
AN:  083102786
UD:  198700

Record 57 of 76 in BIOSIS Previews Part 1 (1987)

TI:  The interoceptive discriminative stimuli induced by the novel putative anxiolytic TVX Q 7821: Behavioral evidence for the specific involvement of serotonin 5-HT-1A receptors.
AU:  SPENCER-D-G-JR; TRABER-J
CS:  Neurobiol. Dep., Troponwerke, Neurather Ring 1, D-5000 Cologne 80, W. Ger
SO:  PSYCHOPHARMACOLOGY 91(1): 25-29
PY:  1987
LA:  English
AB:  TVX Q 7821 is active in several behavioral models of anxiety in animals and has a high selective affinity for brain serotonin 5-HT-1A receptors in binding assays. In order to determine if interaction with 5-HT-1A receptors is important for some of the behavioral effects of this compound, 11 rats were trained to reliably discriminate the interoceptive stimuli induced by TVX Q 7821 (10 mg/kg, IP) from those of saline. Following discrimination acquisition TVX Q 7821 administration resulted in drug-appropriate responding with an ED-50 of 1.5 mg/kg, as did other substances with high affinity for the 5-HT-1A receptor: 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT, ED-50 = 0.16 mg/kg), 5-methoxy-N,N-dimethyltryptamine (5-OMe-DMT, ED-50 = 2.5 mg/kg), buspirone (ED-50 = 5.4 mg/kg). Anxiolytics not acting via the 5-HT-1A receptor, like diazepam and pentobarbital, did not induce full TVX Q 7821-appropriate responses. In addition non-selective 5-HT agonist and antagonists such as bufotenin, quipazine, and methysergide, as well as substances with high affinity for the 5-HT-1B receptor (m-trifluoromethylphenylpiperazine, TFMPP; 5-methoxy-3(1,2,3,6-tetrahydropyridine-4-yl)-1H-indole succinate, RU 24969) did not substitute for TVX Q 7821. These data support a selective 5-HT-1a mechanism of action in vivo for TVX Q 7821 and indicate the suitability of TVX Q 7821 for the investigation of behavioral correlates of the 5-HT-1A receptor.
AN:  083090051
UD:  198700

Record 58 of 76 in BIOSIS Previews Part 2 (1986)

TI:  Brief evaluation of the cutaneous secretion of amphibians.
AU:  Toledo-R-C-D
SO:  Ciencia e Cultura  (Sao Paulo) 38(2): 279-284
PY:  1986
LA:  Portuguese
AN:  031091652
UD:  198600

Record 59 of 76 in BIOSIS Previews Part 2 (1986)

TI:  The relationship between the interceptive stimuli produced by 5-methoxy-N,N-dimethyltryptamine and the serotonin 5-hydroxytryptamine-1 receptor.
AU:  Spencer-D-G-Jr; Glaser-T; Traber-J
CS:  Neurobiol. Dep., Troponwerke, Neurather Ring 1, 5000 Koeln 80, FRG
SO:  Naunyn-Schmiedeberg's Archives of Pharmacology 330 (SUPPL.): R66
MT:  Joint Meeting of the Belgian, Dutch and German Pharmacological and Toxicological Societies, Aachen, West Germany, Sept. 23-26, 1985. NAUNYN-SCHMIEDEBERG'S ARCH PHARMACOL
PY:  1985
LA:  English
AN:  030093867
UD:  198600

Record 60 of 76 in BIOSIS Previews Part 2 (1986)

TI:  Bufotenine antagonizes serotonin's effects on Hermissenda type B photoreceptors.
AU:  Wu-R; Farley-J
CS:  Program Neurosci., Princeton Univ., Princeton, N.J. 08540
SO:  Society for Neuroscience Abstracts 11(1): 575
MT:  15th Annual Meeting of the Society for Neuroscience, Part 1, Dallas, Tex., USA, Oct. 20-25, 1985. SOC NEUROSCI ABSTR
PY:  1985
LA:  English
AN:  030085044
UD:  198600

Record 61 of 76 in BIOSIS Previews Part 2 (1986)

TI:  Selective labeling of serotonin 1A and serotonin 1B binding sites in bovine brain.
AU:  Peroutka-S-J
CS:  Dep. Neurol., Stanford Univ. Med. Cent., Stanford, Calif. 94305, USA
SO:  Brain Research 344(1): 167-171
PY:  1985
LA:  English
AN:  030002240
UD:  198600

Record 62 of 76 in BIOSIS Previews Part 1 (1986)

TI:  Artifactual high-affinity and saturable binding of tritiated 5-hydroxytryptamine induced by radioligand oxidation.
AU:  PEROUTKA-S-J; ISON-P-J; LIU-D-U; BARRETT-R-W
CS:  Dep. Neurol., Stanford Univ. Med. Cent., Stanford, Calif. 94305
SO:  JOURNAL OF NEUROCHEMISTRY 47(1): 38-45
PY:  1986
LA:  English
AB:  The binding of (3H)5-hydroxytryptamine (5-HT, serotonin) to cellular membranes was examined after preincubation of (3H)5-HT in the presence or absence of ascorbate. The tissue preparation was identical in all experiments and consisted of rat cerebellular homogenates in Tris-HCl buffer with 0.1% ascorbate. Cerebellar membranes were used because of their low density of 5-HT-1, binding sites. In the presence of ascorbate during a 4-h preincubation period, minimal specific binding of 2 nM (3H)5-HT is detected. Similar results are obtained with equimolar concentrations of other antioxidants (butylated hydroxytoluene, sodium dithionite, and sodium metabisulfite). Apparent specific binding increased 14-fold following a 4-h preincubation of (3H)-5-HT in the absence of ascorbate. The increase in apparent specific (3H)5-HT binding is time-dependent and plateaus after 4-6 h of preincubation. When ascorbate is present during the 4-h preincubation, Scathcard analysis of (3H)5-HT binding reveals a K-D value of 3.0 +- 0.3 nM and a B-max value of 1.9 +- 0.2 pmol/g tissue. When ascorbate is absent during the preincubation, the K-D is essentially unchanged at 3.6 +- 0.1 nM but the B-max is significantly increased to 36.5 +- 7 pmol/g tissue. Drug competition studies reveal that the apparent specific "(3H)5-HT binding" in the absence of ascorbate appears to be displaced by nanomolar concentrations of hydroxylated tryptamines (5-HT, bufotenine) but not by nonhydroxylated tryptamines (5-methoxytryptamine, tryptamine). HPLC analysis demonstrates that (3H)5-HT is essentially destroyed by a 4-h incubation of 22 degree C in the absence of ascorbate. We conclude that oxidation of (3H)5-HT prior to the addition of membrane homogenates leads to the detection of an artifactual high-affinity and saturable "(3H)5-HT binding site" that appears to have a distinct pharmacological profile. The capacity of other ligands to compete for this binding site is related to their potential as antioxidants and not to their affinity for a novel !
membrane recognition site labeled by (3H)5-HT.
AN:  082065644
UD:  198600

Record 63 of 76 in BIOSIS Previews Part 1 (1986)

TI:  Indolealkylamines and prolactin secretion: A structure-activity study in the central nervous system of the rat.
AU:  SEEMAN-G; BROWN-G-M
CS:  Dep. Neurosciences, McMaster Univ., Hamilton, Ont., Can
SO:  NEUROPHARMACOLOGY 24(12): 1195-1200
PY:  1985
LA:  English
AB:  The present study was performed to examine the central effects of the indolealkylamine hallucinogens, 5-methoxy-N,N-dimethyltryptamine (MDMT), bufotenin and N,N-dimethyltryptamine (DMT), infused intracerebroventricularly (i.c.v.) into the lateral ventricle. They were found to have a stimulatory effect upon the secretion of prolactin. Their order of potency was compared. From a structure-activity point of view, MDMT is the most potent, followed by bufotenin, and then by DMT. Bufotenin, which does not readily cross the blood-brain barrier, caused a prolonged effect on the elevation of prolactin, with a suggestion of a biphasic effect at the maximum dose (0.02 M). N,N-dimethyltryptamine showed a clear dose-response relationship in the stimulation of the release of prolactin. The present results confirm those of previous investigators, who have demonstrated that these drugs cause the release of prolactin, with a possible biphasic effect. The present results suggest that, the response which was obtained was centrally mediated, and probably did not involve stimulation of peripheral receptors and the time course of action of indoles is different when infused centrally, compared to their time course when infused peripherally.
AN:  081085435
UD:  198600

Record 64 of 76 in BIOSIS Previews Part 1 (1986)

TI:  Bufotenine reconsidered.
AU:  MCLEOD-W-R; SITARAM-B-R
CS:  46 Bowen Crescent, Nort Carlton, Victoria, 3054, Australia
SO:  ACTA PSYCHIATRICA SCANDINAVICA 72(5): 447-450
PY:  1985
LA:  English
AB:  Bufotenine given intravenously to a medically trained volunteer subject correlated with the appearance of profound perceptual and emotional changes which were of short duration. The compound rapidly disappeared from the blood and metabolites quickly appeared in the urine of the subject.
AN:  081075809
UD:  198600

Record 65 of 76 in BIOSIS Previews Part 1 (1986)

TI:  Carbon-11 labeling of indolealkylamine alkaloids and the comparative study of their tissue distributions.
AU:  TAKAHASHI-T; TAKAHASHI-K; IDO-T; YANAI-K; IWATA-R; ISHIWATA-K; NOZOE-S
CS:  Div. Radioisotope Res., Cyclotron Radioisotope Cent., Tohoku Univ., Aoba, Aramaki, Sendai 980, Jpn
SO:  INTERNATIONAL JOURNAL OF APPLIED RADIATION AND ISOTOPES 36(12): 965-970
PY:  1985
LA:  English
AB:  Five indoleakkylamines (N,N-dimethyltryptamine, N-methyltryptamine, bufotenine, O-methylbufotenine, N,N,N-trimethyltryptamine iodide) were labeled with 14C by use of 11CH-3I. The labeled compounds were synthesized with a radiochemical yield of 2-50% (based on trapped 11CH-3I) in 20-35 min with radiochemical purities of more than 92%. The tissue distributions of these labeled compounds were investigated in rats. In all cases, the accumulations in the liver, lung and small intestine were high. (11C)DMT and (11C)OMB also accumulated to a large extent in the brain, where their accumulation was retained. Brain uptake of three other radiopharmaceuticals was low. (11C)DMT is the radiopharmaceutical of choice for the study of the serotonin action mechanism in the brain, because it has the highest radiochemical yield and the highest brain uptake of these 11C-labeled compounds.
AN:  081065684
UD:  198600

Record 66 of 76 in BIOSIS Previews Part 1 (1986)

TI:  Serotonin inhibits acetylcholine release from rat striatum slices: Evidence for a presynaptic receptor-mediated effect.
AU:  GILLET-G; AMMOR-S; FILLION-G
CS:  Unite de Pharmacologie et de Toxicologie, Institut Pasteur, 28, rue du Dr. Roux, F 75724 Paris Cedex 15, France
SO:  JOURNAL OF NEUROCHEMISTRY 45(6): 1687-1691
PY:  1985
LA:  English
AB:  Rat brain striatum slices were incubated with (3H)choline, perfused with a physiological buffer, and stimulated by perfusion with a K+-enriched buffer for 2 min. The tritium overflow evoked by K+ was decreased by 5-hydroxytryptamine (serotonin, 5-HT) (maximal inhibition 10-6 M). This effect of 5-HT was mimicked by several agonists (5-methoxytryptamine, N,N-dimethyltryptamine, bufotenin) and blocked by serotonergic antagonists (methiothepin, methysergide, cinanserin) but not by haloperidol; methiothepin and methysergide alone slightly increased the K+-evoked overflow of tritium (3H). Inhibition of the tritium release by 5-HT was not suppressed in the presence of tetrodotoxin (TTX) (10-6 M). These results suggest that 5-HT tonically inhibits acetylcholine (ACh) release from striatal cholinergic neurons by acting on a presynaptic receptor localized on cholinergic terminals.
AN:  081045676
UD:  198600

Record 67 of 76 in BIOSIS Previews Part 1 (1986)

TI:  Multiple high affinity binding sites for 5-hydroxytryptamine: A new class of sites distinct from 5 HT-1 and S-2.
AU:  ROBAUT-C; FILLION-M-P; DUFOIS-S; FAYOLLE-BAUGUEN-C; ROUSSELLE-J-C; GILLET-G; BENKIRANE-S; FILLION-G
CS:  Unite de Pharmacologie, Institut Pasteur, 28 rue du Dr. Roux, F75724 Paris Cedex 15, France
SO:  BRAIN RESEARCH 346(2): 250-262
PY:  1985
LA:  English
AB:  Two different classes of binding sites probably related to serotonergic receptors have already been reported: 5-HT-1 binding sites recognize (3H)5-hydroxytryptamine with a high affinity (K-d = 3 nM) and S-2 binding sites recognize (3H)spiroperidol and (3H)ketanserine. An additional population of sites has been observed in crude membrane preparations or fractions enriched with synaptosomal membranes obtained from rat brain cortex. This population was observed as a single class of sites in a synaptosomal fraction (L fraction-according to Laduron (1977)). It corresponded to a dissociation constant K-d = 13-15 nM, and B-max = 0.80 +- 0.15 pmol/mg protein. Displacement experiments showed that it recognized preferentially the 5-HT structure (bufotenin, 5-MeO-tryptamine). Tryptamine was a weak displacer and 5,7-dihydroxytryptamine totally inefficient. Neither 8-OH-DPAT, nor quipazine had any effect. Methiothepin, cinanserin and cyproheptadine displaced 5-HT from these sites whereas ergot derivatives did not. Contrary to 5-HT-1 binding, this recently observed binding was not altered by GTP; alpha-MSH reduced the corresponding B-max whereas Leu-enkephalin did not. The degenerative lesion of the serotonergic fibers led to a slight increase in the B-max of the binding without altering the K-d which means that corresponding sites are not located on serotonergic fibers and might be postsynaptically located.
AN:  081045626
UD:  198600

Record 68 of 76 in BIOSIS Previews Part 2 (1985)

TI:  Cyproheptadine reduces or prevents ischemic central nervous system damage.
AU:  Zivin-J-A
CS:  Dep. Neurology, Univ. Mass. Med. Center, 55 Lake Ave. North, Worcester, MA 01605
SO:  Neurology 35(4): 584-587
PY:  1985
LA:  English
AN:  029011600
UD:  198500

Record 69 of 76 in BIOSIS Previews Part 2 (1985)

TI:  Carbon-11-labeled indolealkylamines as potential serotonin-1 receptor mapping agents: Synthesis and biodistribution.
AU:  Yanai-K; Takahashi-K; Ishiwata-K; Takahashi-T; Kawashima-K; Iwata-R; Ido-T
CS:  Cyclotron and Radioisotope Center, Tohoku University, Aramaki, Sendai-shi, 980 Japan
SO:  Journal of Labelled Compounds and Radiopharmaceuticals 21(11-12): 1152-1154
MT:  5th International Symposium on Radiopharmaceutical Chemistry, Tokyo, Japan, July 9-13, 1984. J LABELLED COMPD RADIOPHARM
PY:  1984
LA:  English
AN:  028089117
UD:  198500

Record 70 of 76 in BIOSIS Previews Part 2 (1985)

TI:  Identification of 5-(beta-D-glucopyranuronosyloxy)-N,N-dimethyltryptamine as a metabolite of bufotenine in the rabbit.
AU:  Vigdorchik-M-N; Turchin-K-F; Gus'kova-T-A; Yakubovich-L-M; Krasavina-L-S; Lukin-O-V; Lutsenko-N-G; Suvorov-N-N
CS:  O. Ordzhonikidze All-Union Scientific-Research Inst. Pharmaceutical Chemistry, Moscow
SO:  Soviet Journal of Bioorganic Chemistry 10(2): 148-152
PY:  1984
LA:  English
AN:  028046790
UD:  198500

Record 71 of 76 in BIOSIS Previews Part 1 (1985)

TI:  5-Hydroxytryptamine receptor in isolated rabbit aorta: Characterization with tryptamine analogs.
AU:  CLANCY-B-M; MAAYANI-S
CS:  Department of Pharmacology, Mount Sinai School of Medicine of the City University of New York, 1 Gustave L. Levy Place, New York, N.Y. 10029
SO:  JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS 233(3): 761-769
PY:  1985
LA:  English
AB:  The 5-HT-2 (5-hydroxytryptamine) receptor in isolated rabbit thoracic aorta was characterized by examining the relationships between structure and activity of 9 tryptamine analogs. All assays were conducted after blockade of the alpha-adrenergic receptor and inactivation of the neuronal uptake-1 system and monoamine oxidase. Seven of the analogs tested were agonists. 6-Hydroxytryptamine and 7-hydroxytryptamine showed little or no agonist activity in this preparation. The pA-2 (partial antagonism) of spiperone was independent of the agonist assayed and defined the receptor activated by each agonist as the 5-HT-2 receptor. The dissociation constant (K-A) and relative intrinsic efficacy were determined for each agonist. The K-A and relative intrinsic efficacy values for 5-hydroxytryptamine were 0.25 muM and 1, respectively. The K-A and relative intrinsic efficacy values for 5-methoxytryptamine were 0.14 muM and 0.86, respectively, and were not significantly different from those for 5-hydroxytryptamine. The other 5 analogs were partial agonists. N-Methyl-5-hydroxytryptamine and bufotenine had relative intrinsic efficacies of about 0.3 and K-A values not statistically different from the K-A value for 5-hydroxytryptamine. Tryptamine, 5-methyltryptamine and alpha-methyl-tryptamine had K-A values of about 1 muM and relatie intrinsic efficacies of 0.6, 0.6 and 0.4, respectively. The differential effects of structural changes on drug affinity and intrinsic efficacy were illustrated. This information will be applicable in the design of selective agonists or antagonists for the classification of less well defined 5-hydroxytryptamine receptors.
AN:  080056276
UD:  198500

Record 72 of 76 in BIOSIS Previews Part 1 (1985)

TI:  Isolation of the alkaloids and evaluation of the diuretic activity of Arundo donax.
AU:  WASSEL-G-M; AMMAR-N-N
CS:  Pharmaceutical Sci. Lab. National Res. Cent., Tahrir St. Dokki Cairo-Egypt
SO:  FITOTERAPIA 55(6): 357-358
PY:  1984
LA:  English
AB:  From the aerial parts and rhizomes of Arundo donax the following alkaloids were isolated; N,N-dimethyltryptamine, 5-methoxy-N-methyltryptamine, bufotenine from both aerial parts and rhizomes, gramine from the aerial parts, bufotenidine and dehydrobufotenine from the rhizomes. The extract of the rhizomes showed a significant diuretic activity (in rats).
AN:  080053001
UD:  198500

Record 73 of 76 in BIOSIS Previews Part 1 (1985)

TI:  Long-lasting effects of intrauterine growth retardation of basal and 5-hydroxytryptamine stimulated (sodium, potassium)-ATPase in the brain of developing rats.
AU:  CHANEZ-C; FLEXOR-M-A; HAMON-M
CS:  INSERM U 29, Cent. Recherches Biol. Dev. Foetal Neonatal, Association Claude Bernard, Hop. Port-Royal, 123, Blvd. Port-Royal, 75674 Paris Cedex 14
SO:  NEUROCHEMISTRY INTERNATIONAL 7(2): 319-330
PY:  1985
LA:  English
AB:  Intrauterine growth retardation induced by ligation of the uterine vessels in pregnant rats on the 5th day before delivery was associated with brain and body weights of hypotrophic offspring significantly lower than those of pair-aged control rats, even after 6 wk of postnatal rearing under normal conditions. In vitro measurements in homogenates indicated that Na+/K+-ATPase in the forebrain, cerebellum and hippocampus was less active in hypotrophic rats than in pair-aged controls for at least the 1st mo. after birth. 5-HT (5-hydroxytryptamine) and related agonists (RU-24969 (5-methoxy-3-(1,2-3,6-tetrahydro-4-pyridinyl)-IH-indolesuccinate), butotenine and to a lower extent, tryptamine) stimulated Na+/K+-ATPase activity more efficiently in tissues from hypotrophic rats than in those from control animals. Opposite changes were noted in the brain stem: basal Na+/K+-ATPase activity was higher in hypotrophic rats during the 2nd half of the 1st postnatal month but the stimulatory effect of 5-HT was lower than in pair-aged control animals. Since potent 5-HT antagonists such as cinanserin, methiothepin and methysergide, prevented the 5-HT induced-activation of Na+/K+-ATPase in brain homogenates, these results are discussed in relation with the possible existence of a specific 5-HT receptor controlling Na+/K+-ATPase activity in the rat brain.
AN:  080042472
UD:  198500

Record 74 of 76 in BIOSIS Previews Part 1 (1985)

TI:  Guanine nucleotides modulate cortical S-2 serotonin receptors.
AU:  TITELER-M; BATTAGLIA-G; SHANNON-M
CS:  Nova Pharmaceuticals, Wade Ave., P.O. Box 21204, Baltimore, Md. 21228
SO:  JOURNAL OF RECEPTOR RESEARCH 4(7): 705-712
PY:  1984
LA:  English
AB:  Many radiolabeled receptors coupled to intracellular adenylate cyclase activity are modulated by physiological modulators such as GTP and Gpp(NH)p (guanosine imidodiphosphate). The apparent affinity of agonists competing for the binding of 3H-antagonist-labeled receptors is reduced in the presence of GTP and Gpp(NH)p. The agonist-specific effects of GTP and Gpp(NH)p on rat brain cortical S-2 serotonin receptors are reported. The agonists serotonin, 5-methoxytryptamine, bufotenine and tryptamine display 3-fold lower affinities for S-2 serotonin receptors in the presence of 10-4 M GTP or Gpp(NH)p than in the absence of the nucleotides. The antagonists spiperone, cinanserin, cyproheptadine and methysergide are unaffected by the guanine nucleotides. The Hill coefficients of the agonists increase from between 0.70-0.80 to 0.90-1.00 due to guanine nucleotides. ATP, ADP and GDP have little or no effect. This pattern of guanine nucleotide effects was found with receptors which are modulated by a guanine nucleotide regulatory protein and may indicate that the S-2 serotonin receptor may be coupled to intracellular adenylate cyclase activity.
AN:  079080212
UD:  198500

Record 75 of 76 in BIOSIS Previews Part 1 (1985)

TI:  5-hydroxytryptamine antagonists and blockade of neuronal (5-hydroxytryptamine) receptors on ganglion cells.
AU:  NASH-H-L; WALLIS-D-I; ASH-G
CS:  Department Physiology, University College, P.O. Box 78, Cardiff, CF1 1XL, U.K
SO:  GENERAL PHARMACOLOGY 15(4): 339-344
PY:  1984
LA:  English
AB:  Potential changes in superior cervical ganglion cells evoked by 5-HT (5-hydroxytryptamine) or the nicotinic agonist, dimethyl-phenyl piperazinium (DMPP), were recorded using the sucrose-gap method and a number of putative 5-HT antagonists tested for potency and selectivity. Selective blockade of 5-HT responses was produced by 5-HT itself and, in increasing order of potency, by cocaine, metoclopramide and quipazine. A non-selective blockade was observed with bufotenine and d-tubocurarine. Substances which had no effect on 5-HT responses included methysergide and other compounds related to LSD, cinanserin, cyproheptadine, phenylbiguanide and morphine. The results provide further information about the 5-HT receptor on sympathetic ganglion cells. This receptor evidently is distinct from neuronal receptors in the myenteric plexus and on cholinergic nerve terminals.
AN:  079043444
UD:  198500

Record 76 of 76 in BIOSIS Previews Part 1 (1985)

TI:  Identification of N,N-dimethyl-O-(beta-D-glucopyranuronosyl)-5-hydroxytryptamine as a bufotenine metabolite in rabbits.
AU:  VIGDORCHIK-M-M; TURCHIN-K-F; GUS'KOVA-T-A; YAKUBOVICH-L-M; KRASAVINA-L-S; LUKIN-O-V; LUTSENKO-N-G; SUVOROV-N-N
CS:  S. Ordzhonikidze All-Union Res. Chem.-Pharm. Inst., Moscow, USSR
SO:  BIOORGANICHESKAYA KHIMIYA 10(2): 260-264
PY:  1984
LA:  Russian
AB:  A bufotenine metabolite was isolated from rabbit urine by column chromatography on cellulose and preparative paper electrophoresis in acidic buffer. It has the structure of N,N-dimethyl-O-(beta-D-glucopyranuronosyl)-5-hydroxytryptamine as proved by comparison of chromatographic, electrophoretic and NMR data with those for synthetic O-glucuronide.
AN:  079006597
UD:  198500