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 DOI: 10.1016/0014-2999(83)90464-8 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Animal drug discrimination study Peer reviewed |
|---|---|
| Population | Rats trained to discriminate DOM from saline |
| Interventions | DOM mescaline LSD 5-OMe DMT quipazine TFMPP RU-24969 ketanserin pirenperone |
| Dose | 1.0 mg/kg DOM |
| Topics | Serotonin |
| Key points | The DOM discriminative stimulus generalized to mescaline, LSD, 5-OMe DMT, and quipazine but not to TFMPP or RU-24969. The 5-HT2 antagonists ketanserin and pirenperone blocked DOM's effects, and pirenperone also blocked generalization to the other hallucinogens and quipazine. The authors suggest these effects may involve 5-HT2 serotonin receptor sites labeled by tritiated ketanserin. |
Abstract
Rats trained to discriminate 1.0 mg/kg of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) from saline in a two-lever operant choice task were administered doses of mescaline, LSD, 5-methoxy-N,N-dimethyltryptamine (5-OMe DMT), quipazine, TFMPP and RU-24969. The DOM-stimulus generalized to the three hallucinogenic agents and to quipazine, but not to the purported serotonin agonists TFMPP or RU-24969. Pretreatment of the animals with the 5-HT2 antagonists ketanserin and pirenperone antagonized the effect produced by DOM. Pirenperone also blocked DOM-stimulus generalization to mescaline, LSD, 5-OMe DMT and quipazine. The results of this study suggest that the discriminative stimulus effects of DOM, the three hallucinogenic agents to which DOM-stimulus generalization occurred, and quipazine, may involve those sub-populations of serotonin receptors that are labeled by tritiated ketanserin (i.e. 5-HT2 sites).
Comparable studies
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| 3,4-Methylenedioxymethamphetamine and 3,4-methylenedioxyamphetamine destroy serotonin terminals in rat brain: quantification of neurodegeneration by measurement of [3H]paroxetine-labeled serotonin uptake sites. Rat brain | 1987 | Animal experiment | |
| Comparison of the monoamine transporters from human and mouse in their sensitivities to psychostimulant drugs Human and mouse dopamine, norepinephrine, and serotonin transporters expressed in cells | 2006 | In vitro laboratory study |
Citations in the library
Cited by 87
- Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents. Life Sciences December 17, 1984
- Differences Between the Mechanism of Action of MDMA, MBDB, and the Classic Hallucinogens. Identification of a New Therapeutic Class: Entactogens Journal of Psychoactive Drugs October 1, 1986
- Classic psychedelics: An integrative review of epidemiology, therapeutics, mystical experience, and brain network function. Pharmacology & Therapeutics May 1, 2019
- Psychedelics and the Human Receptorome PLoS One 2010
- The hallucinogenic world of tryptamines: an updated review. Archives of Toxicology August 1, 2015
and 82 more in the library
Cites 3
- A behavioural and biochemical study in rats of 5-hydroxytryptamine receptor agonists and antagonists, with observations on structure-activity requirements for the agonists. British Journal of Pharmacology July 1, 1981
- Comparison of behavioral properties of di- and tri-methoxyphenylisopropylamines. Pharmacology, Biochemistry, and Behavior October 1982
- The discriminative stimulus properties of 2,5-dimethoxy-4-methylamphetamine (DOM): differentiation from amphetamine. Psychopharmacology 1980