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 o...

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Bibliographic Details
Main Authors: Yamakuni Hisashi (Author), Nakayama Hiroe (Author), Matsui Shigeo (Author), Imazumi Katsunori (Author), Matsuo Masahiko (Author), Mutoh Seitaro (Author)
Format: Book
Published: Elsevier, 2006-01-01T00:00:00Z.
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Summary: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 by cisplatin (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. Keywords:: 5-HT4 receptor, 5-HT3 receptor, delayed emesis
Item Description:1347-8613
10.1254/jphs.SCJ050070