Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents.
Richard A Glennon, M Titeler, J D Mckenney
Life Sciences December 17, 1984 DOI: 10.1016/0024-3205(84)90436-3 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Observational study Peer reviewed |
|---|---|
| Citations | 636 |
| Key findings | Binding affinities of psychoactive agents for 5-HT2 receptors strongly correlate with their hallucinogenic potencies in humans and with behavioral effects in animals. |
Abstract
The affinities (Ki values) of twenty two psycho-active agents, including LSD, 5-OMe DMT and a series of phenalkylamine derivatives, for cortical 5-HT1 and 5-HT2 binding sites were compared with two measures of behavioral activity. It was found that a significant correlation (r = 0.938) exists between the 5-HT2 binding affinities of these agents and their ED50 values as determined in tests of stimulus generalization using 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) as the training drug. Furthermore, for fifteen of these agents where human data were available, a significant correlation (r = 0.924) also exists between 5-HT2 binding affinities and their human hallucinogenic potencies. The results of this study suggest that the mechanism of action of these agents involves 5-HT2-related events.
In the evidence
This study is part of the evidence base for a synthesis in the library. Here is how each one recorded it.
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State of the evidence: Serotonin Supports
5-HT2 binding affinities of psychoactive agents correlated strongly with hallucinogenic potency in humans (r = 0.924) and with animal behavioral effects.
Synthesized
Citations in the library
Cited by 334
- The entropic brain: a theory of conscious states informed by neuroimaging research with psychedelic drugs Frontiers in Human Neuroscience 2014
- Neural correlates of the psychedelic state as determined by fMRI studies with psilocybin Proceedings of the National Academy of Sciences January 23, 2012
- Human hallucinogen research: guidelines for safety. Journal of Psychopharmacology July 1, 2008
- Psilocybin occasioned mystical-type experiences: immediate and persisting dose-related effects. Psychopharmacology December 1, 2011
- Mystical experiences occasioned by the hallucinogen psilocybin lead to increases in the personality domain of openness Journal of Psychopharmacology September 28, 2011
and 329 more in the library
Cites 4
- Stereospecific binding ofd-lysergic acid diethylamide (LSD) to brain membranes: Relationship to serotonin receptors Brain Research September 1, 1975
- Serotonin Receptor Binding Affinities of Several Hallucinogenic Phenylalkylamine and N,N-Dimethyltryptamine Analogues Journal of Medicinal Chemistry 1978
- Antagonism of the effects of the hallucinogen DOM and the purported 5-HT agonist quipazine by 5-HT2 antagonists. European Journal of Pharmacology July 1, 1983
- The discriminative stimulus properties of 2,5-dimethoxy-4-methylamphetamine (DOM): differentiation from amphetamine. Psychopharmacology 1980