Zacopride was found to significantly increasealdosterone levels in human subjects for 180 minutes at a dose of 400 micrograms. It is thought to do this by stimulating the 5-HT4 receptors on the adrenal glands. Zacopride also stimulated aldosterone secretion when applied to human adrenal glandsin vitro. No significant changes were observed inrenin,ACTH, orcortisol levels.[2]
Zacopride has been tested in clinical trials for the treatment ofschizophrenia, but was found unsuccessful.[10]
^abLefebvre H, Contesse V, Delarue C, Soubrane C, Legrand A, Kuhn JM, et al. (December 1993). "Effect of the serotonin-4 receptor agonist zacopride on aldosterone secretion from the human adrenal cortex: in vivo and in vitro studies".The Journal of Clinical Endocrinology and Metabolism.77 (6):1662–6.doi:10.1210/jcem.77.6.8263156.PMID8263156.
^Costall B, Domeney AM, Gerrard PA, Kelly ME, Naylor RJ (April 1988). "Zacopride: anxiolytic profile in rodent and primate models of anxiety".The Journal of Pharmacy and Pharmacology.40 (4):302–5.doi:10.1111/j.2042-7158.1988.tb05254.x.PMID2900320.S2CID1083706.
^Fontana DJ, Daniels SE, Eglen RM, Wong EH (March 1996). "Stereoselective effects of (R)- and (S)-zacopride on cognitive performance in a spatial navigation task in rats".Neuropharmacology.35 (3):321–7.doi:10.1016/0028-3908(96)00191-8.PMID8783207.S2CID12818436.
^Young R, Johnson DN (August 1991). "Anxiolytic-like activity of R(+)- and S(-)-zacopride in mice".European Journal of Pharmacology.201 (2–3):151–5.doi:10.1016/0014-2999(91)90338-Q.PMID1686755.
^Carley DW, Depoortere H, Radulovacki M (2001). "R-zacopride, a 5-HT3 antagonist/5-HT4 agonist, reduces sleep apneas in rats".Pharmacology, Biochemistry, and Behavior.69 (1–2):283–9.doi:10.1016/S0091-3057(01)00535-4.PMID11420096.S2CID11848748.
^Meyer LC, Fuller A, Mitchell D (February 2006). "Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats".American Journal of Physiology. Regulatory, Integrative and Comparative Physiology.290 (2): R405-13.doi:10.1152/ajpregu.00440.2005.PMID16166206.S2CID224414.
^Knapp DJ, Pohorecky LA (April 1992). "Zacopride, a 5-HT3 receptor antagonist, reduces voluntary ethanol consumption in rats".Pharmacology, Biochemistry, and Behavior.41 (4):847–50.doi:10.1016/0091-3057(92)90237-A.PMID1594653.S2CID45436887.
^Newcomer JW, Faustman WO, Zipursky RB, Csernansky JG (September 1992). "Zacopride in schizophrenia: a single-blind serotonin type 3 antagonist trial".Archives of General Psychiatry.49 (9):751–2.doi:10.1001/archpsyc.1992.01820090079013.PMID1514881.
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