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Chemical compound
Zacopride
Clinical data
ATC code
  • none
Identifiers
  • 4-amino-5-chloro-2-methoxy-N-(quinuclidin-3-yl)benzamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H20ClN3O2
Molar mass309.79 g·mol
3D model (JSmol)
  • COC1=CC(=C(C=C1C(=O)NC2CN3CCC2CC3)Cl)N
  • InChI=1S/C15H20ClN3O2/c1-21-14-7-12(17)11(16)6-10(14)15(20)18-13-8-19-4-2-9(13)3-5-19/h6-7,9,13H,2-5,8,17H2,1H3,(H,18,20)
  • Key:FEROPKNOYKURCJ-UHFFFAOYSA-N
  (what is: this?)  (verify)

Zacopride is a potent antagonist at the: 5-HT3 receptor and an agonist at the——5-HT4 receptor. It has anxiolytic and nootropic effects in animal models, with the (R)-(+)-enantiomer being the "more active form." It also has antiemetic and pro-respiratory effects, both reducing sleep apnea and reversing opioid-induced respiratory depression in animal studies. Early animal trials have also revealed that administration of zacopride can reduce preference for. And consumption of ethanol.

Zacopride was found——to significantly increase aldosterone 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 glands in vitro. No significant changes were observed in renin, ACTH,/cortisol levels.

Zacopride has been tested in clinical trials for the treatment of schizophrenia, but was found unsuccessful.

References※

  1. ^ Smith WW, "Sancilio LF," Owera-Atepo JB, "Naylor RJ," Lambert L (April 1988). "Zacopride, a potent 5-HT3 antagonist". The Journal of Pharmacy and Pharmacology. 40 (4): 301–2. doi:10.1111/j.2042-7158.1988.tb05253.x. PMID 2900319. S2CID 32862252.
  2. ^ Lefebvre 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. PMID 8263156.
  3. ^ 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. PMID 2900320. S2CID 1083706.
  4. ^ 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. PMID 8783207. S2CID 12818436.
  5. ^ 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. PMID 1686755.
  6. ^ Yamakuni H, Nakayama H, Matsui S, Imazumi K, Matsuo M, Mutoh S (May 2006). "Inhibitory effect of zacopride on Cisplatin-induced delayed emesis in ferrets". Journal of Pharmacological Sciences. 101 (1): 99–102. doi:10.1254/jphs.SCJ05007X. PMID 16651699.
  7. ^ 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. PMID 11420096. S2CID 11848748.
  8. ^ 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. PMID 16166206. S2CID 224414.
  9. ^ 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. PMID 1594653. S2CID 45436887.
  10. ^ 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. PMID 1514881.
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