Quipazine produces a head-twitch response and other psychedelic-consistent effects in animal studies including in mice, rats, and monkeys.[1][3][9][10][11] These effects appear to be mediated by activation of the serotonin 5-HT2A receptor, as they are blocked by serotonin 5-HT2A receptor antagonists like ketanserin.[1][3][11] The head twitches induced by quipazine are potentiated by the monoamine oxidase inhibitor (MAOI) pargyline.[11][12] Based on this, it has been suggested that quipazine may act as a serotonin releasing agent and that it may induce the head twitch response by a dual action of serotonin 5-HT2A receptor agonism and induction of serotonin release.[11][12]
Quipazine did not produce psychedelic effects in humans up to a dose of 25mg, which was the highest dose tested due to serotonin 5-HT3 receptor-mediated side effects of nausea and gastrointestinal discomfort.[13][3]Alexander Shulgin has anecdotally claimed that a fully effective psychedelic dose could be reached by blocking serotonin 5-HT3 receptors using the serotonin 5-HT3 receptor antagonistondansetron.[3][14]
Although quipazine does not generalize to dextroamphetamine in drug discrimination tests of dextroamphetamine-trained rodents, dextroamphetamine and cathinone have been found to partially generalize to quipazine in assays of quipazine-trained rodents.[15][16] In relation to this, it has been suggested that quipazine might possess some dopaminergic activity, as the discriminative stimulus properties of amphetamine appear to be mediated by dopamine signaling.[15][16] Relatedly, quipazine has been said to act as a dopamine receptor agonist in addition to serotonin receptor agonist.[11] Conversely however, the generalization may be due to serotonergic activities of amphetamine and cathinone.[17]Fenfluramine has been found to fully generalize to quipazine, but levofenfluramine, in contrast to quipazine, did not generalize to dextroamphetamine.[15][10]
1 2 3 4 5 6 Glennon RA, Dukat M (2 May 2023). "Quipazine: Classical hallucinogen? Novel psychedelic?". Australian Journal of Chemistry. 76 (5): 288–298. doi:10.1071/CH22256. ISSN0004-9425.
1 2 3 4 Cappelli A, Butini S, Brizzi A, Gemma S, Valenti S, Giuliani G, etal. (2010). "The interactions of the 5-HT3 receptor with quipazine-like arylpiperazine ligands: the journey track at the end of the first decade of the third millennium". Curr Top Med Chem. 10 (5): 504–526. doi:10.2174/156802610791111560. PMID20166948.
↑ Rodríguez R, Pardo EG (1971). "Quipazine, a new type of antidepressant agent". Psychopharmacologia. 21 (1): 89–100. doi:10.1007/BF00404000. PMID5567294.
↑ Glennon RA (1996). "Classical Hallucinogens". Pharmacological Aspects of Drug Dependence. Vol.118. Berlin, Heidelberg: Springer Berlin Heidelberg. p.343–371. doi:10.1007/978-3-642-60963-3_10. ISBN978-3-642-64631-7.
1 2 Glennon RA (1988). "Site-Selective Serotonin Agonists as Discriminative Stimuli". Transduction Mechanisms of Drug Stimuli. Berlin, Heidelberg: Springer Berlin Heidelberg. p.15–31. doi:10.1007/978-3-642-73223-2_2. ISBN978-3-642-73225-6.
1 2 3 4 5 Nakagawasai O, Arai Y, Satoh SE, Satoh N, Neda M, Hozumi M, etal. (January 2004). "Monoamine oxidase and head-twitch response in mice. Mechanisms of alpha-methylated substrate derivatives". Neurotoxicology. 25 (1–2): 223–232. doi:10.1016/S0161-813X(03)00101-3. PMID14697897.
1 2 3 Young R, Glennon RA (1986). "Discriminative stimulus properties of amphetamine and structurally related phenalkylamines". Med Res Rev. 6 (1): 99–130. doi:10.1002/med.2610060105. PMID3512936.
1 2 Glennon RA, Rosecrans JA (1981). "Speculations on the mechanism of action of hallucinogenic indolealkylamines". Neurosci Biobehav Rev. 5 (2): 197–207. doi:10.1016/0149-7634(81)90002-6. PMID7022271.
↑ Goudie AJ (September 1985). "Comparative effects of cathinone and amphetamine on fixed-interval operant responding: a rate-dependency analysis". Pharmacol Biochem Behav. 23 (3): 355–365. doi:10.1016/0091-3057(85)90006-1. PMID4048231.
↑ DE 2006638,Rodriguez R,issued 1970 Chem. Abstr., 73: 98987g (1970).
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