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Zacopride
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| Systematic (IUPAC) name | |
| 4-amino-N-(1-azabicyclo[2.2.2]octan-8-yl)-5-chloro-2-methoxybenzamide | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C15H20ClN3O2 |
| Mol. mass | 309.791 g/mol |
| SMILES | & |
| Synonyms | Zacopride |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Zacopride is a potent antagonist at the 5HT3 receptor1 and an agonist at the 5HT4 receptor.2 It has anxiolytic3 and nootropic effects in animal models,4 with the (R) enantiomer being the more active form.5 It also has antiemetic6 and pro-respiratory effects, both reducing sleep apnoea7 and reversing opioid-induced respiratory depression in animal studies.8
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References
- ^ 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
- ^ 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
- ^ 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
- ^ 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
- ^ 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
- ^ 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
- ^ 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
- ^ 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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- This page was last modified on 29 October 2008, at 01:31.
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