Erowid References Database
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Trabucchi M, Hofmann M, Montefusco O, Spano PF.
“Ergot Alkaloids and Cyclic Nucleotides in the CNS”.
Pharmacology. 1978;16(Supp. 1):150-55.
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Abstract
Ergot alkaloids (EAs) and cyclic nucleotides in the CNS are discussed. EAs act through different mechanisms. Neuroleptics block the stimulation of dopaminergic (DA) receptors by LSD while 2-Br-LSD, which is not hallucinogenic in man is not active on DA receptors. Ergotamine (E) and dihydroE block DA induced stimulation of striatal adenylate cyclase (AC) less than apomorphine (A)-induced stimulation. Bromocriptine (B) increases rat striatal cAMP in vivo but blocks in vitro activation of AC by DA. B is therapeutically useful in parkinsonism and Huntingdon's chorea, where it is as efficacious as haloperidol (H). H (2 mg/kg) and reserpine (5 mg/kg) block the increase in cAMP with B (2 mg/kg). B (2 mg/kg), H (2 mg/kg) increases cGMP levels, B and DHergotoxine reduce striatal 3,4-dibydroxy phenilacetic acid (DOPAC) for 4 hr. Concentrations of EAs which inhibit the binding of 3H-DA in calf caudate membranes are between 40 and 110 nM. All EAs block AC activity even at low concentration (DHergotoxin, 5 x 10 M). An age-related decrease in the sensitivity to DA stimulation of AC in striatum, substantia nigra and DAergic areas of rats has been shown.
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