Inhibitory effect of zacopride on Cisplatin-induced delayed emesis in ferrets.

Abstract

We evaluated the antiemetic effect of zacopride, a potent 5-HT3-receptor antagonist with 5-HT4-receptor agonist properties, on delayed emesis caused by cisplatin (5 mg/kg, i.p.) in ferrets, compared with granisetron, a selective 5-HT3-receptor antagonist. Multiple intravenous injections of zacopride at 1 mg/kg, a dose that completely inhibited acute emesis caused bycisplatin (10 mg/kg, i.v.), significantly reduced delayed emesis. Granisetron (3.2 mg/kg) also reduced delayed emesis but this failed to reach statistical significance. The present study suggests that a combined 5-HT3-receptor antagonist/5-HT4-receptor agonist, like zacopride, may be useful against both acute and delayed emesis induced by cancer chemotherapy.

• Authors: Hisashi Yamakuni, Hiroe Nakayama, Shigeo Matsui, Katsunori Imazumi, Masahiko Matsuo, Seitaro Mutoh
• Journal: Journal of pharmacological sciences (J Pharmacol Sci) Vol. 101 Issue 1 Pg. 99-102 (May 2006) ISSN: 1347-8613 [Print] Japan
• PMID: 16651699 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Antiemetics
• Antineoplastic Agents
• Benzamides
• Bridged Bicyclo Compounds, Heterocyclic
• Serotonin Antagonists
• zacopride
• Cisplatin
• Granisetron

Topics

• Animals
• Antiemetics (pharmacology)
• Antineoplastic Agents (adverse effects)
• Benzamides (pharmacology)
• Bridged Bicyclo Compounds, Heterocyclic (pharmacology)
• Cisplatin (adverse effects)
• Drug Therapy, Combination
• Ferrets
• Granisetron (pharmacology)
• Male
• Serotonin Antagonists (pharmacology)
• Time Factors
• Vomiting (chemically induced, prevention & control)