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Hallucinogenic drugs are partial agonists of the human platelet shape change response: a physiological model of the 5-HT2 receptor.

S J McClue, C Brazell, S M Stahl

Biological Psychiatry July 1, 1989 DOI: 10.1016/0006-3223(89)90042-5 (opens in new tab)

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AI-extracted from the abstract
Characteristics In vitro pharmacological assay study Peer reviewed
Population Human blood platelets
Interventions 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 mescaline lisuride methysergide lysergic acid cocaine amphetamine phencyclidine
Measures platelet shape change
Topics LSD Serotonin
Keywords Brain Blood platelets Humans Receptors, serotonin Hallucinogens Platelet aggregation Dose-response relationship, drug
Key points Hallucinogens including LSD, N,N-DMT, 5-MeODMT, DOI, bufotenine, and mescaline acted as partial agonists at the platelet 5-HT2 receptor model, whereas structurally similar nonhallucinogens did not. The authors propose that some behavioral effects of LSD-type hallucinogens in humans are due to their actions at 5-HT2 receptors.

Abstract

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-HT2 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-HT2 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, phencyclidine) 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-HT2 receptors and suggests that these hallucinogens are partial 5-HT2 agonists.

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LSD Serotonin 5-MeO-DMT DMT Mescaline