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Vogel WH, Evans BD.
“Structure-Activity-Relationship Of Certain Hallucinogenic Substances Based on Brain Levels”.
Life Sci.. 1977;20(10):1629-36.
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Abstract
A structure-activity-relationship (SAR) for a variety of behaviourally active and inactive compounds, which are naturally occurring or closely structurally related to putative neurotransmitters is reviewed. - The effect of compounds with available brain levels, or: rat conditioned avoidance response (CAR) in the shuttle box was selected for the review. The following compounds shown below are presented, both the actual doses administered (ADA, llmol/kg), and the minimal effective brain level (MEBL-expressed as mol/g brain), at the time an animal first showed a significant reduction in CAR being listed. The SAR within each group of compounds is discussed in relation to these two measurements of potency. A different and new SAR is obtained when MEAL are used, the differences being due to the fate of the substance in the body and its availability to the CNS. Using ADA, LSD, pentamethoxy-PEA, 5-methoxy-DMT and isolysergic acid amide (at doses of 3, 10, 10, and 15'um/kg, respectively), would be the most potent compounds. T. 5-ethoxy T and 5-hydroxy-DMT (with doses of >300, 100 and 100mol/kg, respectively) would rate as weak psychotic compounds. However, using MEBL as the basis for comparison, LSD is still the most potent, but along with 5-methoxy-T (0.5 nmol/g). Compounds slightly less potent are T (after MAO inhibition), pentamethoxy P1SA and 5-hydroxy-DMT (1,1 and 2.5 nmol/g, respectively). As a group, the indolamines show highest potency, the PEAs are next, and the PEOHs are almost devoid of behavioral activity. It is suggested that MEBL be used as the basis of comparison in S-AR studies of behaviorally active substances. Phenylethylamine (PEA) 4-Methoxy-PEA, Tryptamlne (T) 3,4-Dimethoxy-PEA, T (after MAO inhibition) 3,4,5-Trimethoxy-PEA, Dimethyl-T (DMT) 2 4,5-Trimethoxy-PEA, Diethyl-T 2 3,4,5,6-Pentamethoxy-PEA , 5-Methoxy-T - Phenylethanolamine (PEON), 5-Hydroxy-DMT 3,4-Dimethoxy-PEOH, 5-Methoxy-DMT. 3 4,5-Trimethexy-PEOH 3 4-Dimethoxy-N,N-Dimethyl-PEOH, Isolysergic Acid Amide Lysergic Acid Diethylamide Phenylisoproylamine (PIA) 2,4,5-Trimethoxy-PIA 2,3,4-Trimethoxy-PIA
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