Quipazine produces a
head-twitch response and other
psychedelic-consistent effects in animal studies including in mice, rats, and monkeys.[5] However, it failed to produce psychedelic effects in humans at a dose of 25 mg, which was the highest dose tested due to 5-HT3 mediated side effects of
nausea and gastrointestinal discomfort.[6][5] However
Alexander Shulgin claimed that a fully effective psychedelic dose could be reached by blocking 5-HT3 receptors using a
5-HT3 antagonist.[7][5]
^Cappelli A, Giuliani G, Gallelli A, Valenti S, Anzini M, Mennuni L, et al. (May 2005). "Structure-affinity relationship studies on arylpiperazine derivatives related to quipazine as serotonin transporter ligands. Molecular basis of the selectivity SERT/5HT3 receptor". Bioorganic & Medicinal Chemistry. 13 (10): 3455–60.
doi:
10.1016/j.bmc.2005.03.008.
PMID15848758.
^Smith RL, Barrett RJ, Sanders-Bush E (November 1995). "Neurochemical and behavioral evidence that quipazine-ketanserin discrimination is mediated by serotonin2A receptor". The Journal of Pharmacology and Experimental Therapeutics. 275 (2): 1050–7.
PMID7473132.
^Cappelli A, Anzini M, Vomero S, Mennuni L, Makovec F, Doucet E, et al. (February 1998). "Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives". Journal of Medicinal Chemistry. 41 (5): 728–41.
doi:
10.1021/jm970645i.
PMID9513601.
^Cappelli A, Butini S, Brizzi A, Gemma S, Valenti S, Giuliani G, et al. (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): 504–26.
doi:
10.2174/156802610791111560.
PMID20166948.
Quipazine produces a
head-twitch response and other
psychedelic-consistent effects in animal studies including in mice, rats, and monkeys.[5] However, it failed to produce psychedelic effects in humans at a dose of 25 mg, which was the highest dose tested due to 5-HT3 mediated side effects of
nausea and gastrointestinal discomfort.[6][5] However
Alexander Shulgin claimed that a fully effective psychedelic dose could be reached by blocking 5-HT3 receptors using a
5-HT3 antagonist.[7][5]
^Cappelli A, Giuliani G, Gallelli A, Valenti S, Anzini M, Mennuni L, et al. (May 2005). "Structure-affinity relationship studies on arylpiperazine derivatives related to quipazine as serotonin transporter ligands. Molecular basis of the selectivity SERT/5HT3 receptor". Bioorganic & Medicinal Chemistry. 13 (10): 3455–60.
doi:
10.1016/j.bmc.2005.03.008.
PMID15848758.
^Smith RL, Barrett RJ, Sanders-Bush E (November 1995). "Neurochemical and behavioral evidence that quipazine-ketanserin discrimination is mediated by serotonin2A receptor". The Journal of Pharmacology and Experimental Therapeutics. 275 (2): 1050–7.
PMID7473132.
^Cappelli A, Anzini M, Vomero S, Mennuni L, Makovec F, Doucet E, et al. (February 1998). "Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives". Journal of Medicinal Chemistry. 41 (5): 728–41.
doi:
10.1021/jm970645i.
PMID9513601.
^Cappelli A, Butini S, Brizzi A, Gemma S, Valenti S, Giuliani G, et al. (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): 504–26.
doi:
10.2174/156802610791111560.
PMID20166948.