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.