Zacopride

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Zacopride
220px
Systematic (IUPAC) name
4-​amino-​N-​1-​azabicyclo[2.2.2]oct-​3-​yl-​5-​chloro-​2-​methoxybenzamide
Identifiers
CAS Number 90182-92-6
ATC code none
PubChem CID 108182
IUPHAR/BPS 245
Chemical data
Formula C15H20ClN3O2
Molar mass 309.791 g/mol[[Script error: No such module "String".]]
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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]

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. Zacropride also stimulated aldosterone secretion when applied to human adrenal glands in vitro. No significant changes were observed in renin, ACTH, or cortisol levels.[9]

References

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Other respiratory system products (R07)
Lung surfactants
Respiratory stimulants
5-HT4 receptor agonists
BIMU-8 • Zacopride
Other agents for treating respiratory depression

M: RES

anat(n, x, l, c)/phys/devp

proc, drug(R1/2/3/5/6/7)


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  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
  9. ↑ 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
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