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Zacopride: Wikis


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Systematic (IUPAC) name
CAS number 90182-92-6
ATC code none
PubChem 108182
Chemical data
Formula C 15H20ClN3O2  
Mol. mass 309.791 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Zacopride is a potent antagonist at the 5HT3 receptor[1] and an agonist at the 5HT4 receptor.[2] It has anxiolytic[3] and nootropic effects in animal models,[4] with the (R) enantiomer being the more active form.[5] It also has antiemetic[6] and pro-respiratory effects, both reducing sleep apnoea[7] and reversing opioid-induced respiratory depression in animal studies.[8]


  1. ^ Smith WW, Sancilio LF, Owera-Atepo JB, Naylor RJ, Lambert L. Zacopride, a potent 5-HT3 antagonist. Journal of Pharmacy and Pharmacology. 1988 Apr;40(4):301-2. PMID 2900319
  2. ^ Lefebvre H, Contesse V, Delarue C, Soubrane C, Legrand A, Kuhn JM, Wolf LM, Vaudry H. Effect of the serotonin-4 receptor agonist zacopride on aldosterone secretion from the human adrenal cortex: in vivo and in vitro studies. Journal of Clinical Endocrinology and Metabolism. 1993 Dec;77(6):1662-6. PMID 8263156
  3. ^ Costall B, Domeney AM, Gerrard PA, Kelly ME, Naylor RJ. Zacopride: anxiolytic profile in rodent and primate models of anxiety. Journal of Pharmacy and Pharmacology. 1988 Apr;40(4):302-5. PMID 2900320
  4. ^ Fontana DJ, Daniels SE, Eglen RM, Wong EH. Stereoselective effects of (R)- and (S)-zacopride on cognitive performance in a spatial navigation task in rats. Neuropharmacology. 1996 Mar;35(3):321-7. PMID 8783207
  5. ^ Young R, Johnson DN. Anxiolytic-like activity of R(+)- and S(-)-zacopride in mice. European Journal of Pharmacology. 1991 Aug 29;201(2-3):151-5. PMID 1686755
  6. ^ Yamakuni H, Nakayama H, Matsui S, Imazumi K, Matsuo M, Mutoh S. Inhibitory effect of zacopride on Cisplatin-induced delayed emesis in ferrets. Journal of Pharmacological Sciences. 2006 May;101(1):99-102. PMID 16651699
  7. ^ Carley DW, Depoortere H, Radulovacki M. R-zacopride, a 5-HT3 antagonist/5-HT4 agonist, reduces sleep apneas in rats. Pharmacology, Biochemistry and Behaviour. 2001 May-Jun;69(1-2):283-9. PMID 11420096
  8. ^ Meyer LC, Fuller A, Mitchell D. 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. 2006 Feb;290(2):R405-13. PMID 16166206


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