Involvement of 5-HT receptor subtypes in the discriminative stimulus properties of mescaline
James B. Appel, Patrick M. Callahan
European Journal of Pharmacology 1989 DOI: 10.1016/0014-2999(89)90041-1 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Animal experiment Peer reviewed |
|---|---|
| Population | Rats |
| Interventions | mescaline DOM LSD psilocybin 8-OHDPAT RU-24969 TFMPP ketanserin LY-53857 pirenperone metergoline SCH-23390 haloperidol |
| Dose | 10 mg/kg i.p. |
| Topics | Mescaline Psilocybin Serotonin |
| Keywords | Metergoline Pharmacology Haloperidol Stimulus generalization Ketanserin Hallucinogen Ritanserin 5-HT Receptor Butyrophenone |
| Citations | 34 |
| Key findings | 5-HT2 receptors are involved in the stimulus properties of mescaline. |
Abstract
In order to further evaluate the extent to which particular 5-HT receptor subtypes (5-HT1, 5-HT2) might be involved in the behavioral effects of hallucinogenic drugs, rats were trained to discriminate mescaline (10 mg/kg i.p.) from saline and were given substitution (generalization) and combination (antagonism) tests with putatively selective serotonergic and related neuroactive compounds. The mescaline cue generalized to relatively high doses of the 5-HT2 agonists, 2,5-dimethoxy-4-methylamphetamine (DOM), LSD and psilocybin; the extent of generalization to 5-HT1 agonists (8-hydroxy-2-[diethylamino]tetralin (8-OHDPAT), RU-24969 and 8-hydroxy-2-[di-n-propylamino]tetralin (TFMPP] was unclear. Combinations of the training drug and sufficiently high doses of 5-HT2 antagonists (ketanserin, LY-53857, pirenperone) were followed by saline-lever responding; less selective central 5-HT (metergoline), and DA (SCH-23390, haloperidol) antagonists, did not block the mescaline cue. These data suggest that 5-HT2 receptors are involved in the stimulus properties of mescaline.
Comparable studies
Other preclinical and animal studies on mescaline, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Correlation between the potency of hallucinogens in the mouse head-twitch response assay and their behavioral and subjective effects in other species. C57BL/6J mice | 2020 | Experimental study with dose-response experiments | |
| Brain mechanisms of hallucinogens and entactogens Humans and rats | 2001 | Review | |
| Effects of hallucinogenic agents mescaline and phencyclidine on zebrafish behavior and physiology Zebrafish (Danio rerio) | 2012 | Experimental study | |
| Lysergic Acid Diethylamide- and Mescaline-Induced Attenuation of the Effect of Punishment in the Rat Rats | 1976 | Experimental study | |
| Dihydrobenzofuran Analogues of Hallucinogens. 3. Models of 4-Substituted (2,5-Dimethoxyphenyl)alkylamine Derivatives with Rigidified Methoxy Groups Rats (trained to discriminate saline from LSD tartrate) and rat cortical and... | 1996 | In vivo drug discrimination assay and in vitro radioligand binding assay |
Citations in the library
Cited by 18
- The abuse potential of medical psilocybin according to the 8 factors of the Controlled Substances Act Neuropharmacology June 5, 2018
- The hallucinogenic world of tryptamines: an updated review. Archives of Toxicology August 1, 2015
- Psilocybin – Summary of knowledge and new perspectives European Neuropsychopharmacology December 17, 2013
- Synthesis of a Tricyclic Mescaline Analogue by Catalytic C−H Bond Activation Organic Letters March 22, 2003
- Dark Classics in Chemical Neuroscience: Mescaline ACS Chemical Neuroscience May 30, 2018
and 13 more in the library
Cites 9
- Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents. Life Sciences December 17, 1984
- Derivatives of 1-(1,3-benzodioxol-5-yl)-2-butanamine: representatives of a novel therapeutic class Journal of Medicinal Chemistry October 1, 1986
- Neuropharmacological reassessment of the discriminative stimulus properties ofd-lysergic acid diethylamide (LSD) Psychopharmacology 1987
- Mescaline‐induced head‐twitches in the rat: An in vivo method to evaluate serotonin S2 antagonists Drug Development Research 1983
- Role of serotonin in the discriminative stimulus properties of mescaline Pharmacology, Biochemistry, and Behavior May 1, 1975
and 4 more in the library