Improvement of cisplatin-induced emesis and delayed gastric emptying by KB-R6933, a novel 5-HT3 receptor antagonist

被引：27

作者：

Ozaki, A ^{[1
]}

Sukamoto, T ^{[1
]}

机构：

[1] Kanebo Ltd, Pharmaceut R&D Ctr, Miyakojima Ku, Osaka 5348666, Japan

来源：

GENERAL PHARMACOLOGY | 1999年 / 33卷 / 03期

关键词：

KB-R6933; 5-HT3 receptor antagonist; cisplatin; emesis; gastric emptying;

D O I：

10.1016/S0306-3623(98)00286-9

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The effects of a novel 5-hydroxytryptamine(3) (5-HT3) receptor antagonist, KB-R6933, 6-amino5-chloro-1-isopropyl-2-(4-methyl-1-piperazinyl)-benzimidazole dimaleate, on emesis and delayed gastric emptying induced by cisplatin were assessed in experimental models. Prophylactic intravenous or oral treatment with KB-R6933 prolonged the latent period until the first emetic episode and decreased the number of emetic episodes induced by cisplatin in ferrets. KB-R6933 immediately inhibited the subsequent emesis when administered to the ferrets which exhibited established vomiting after administration of cisplatin. In rats treated with cisplatin, the gastric emptying rate was significantly reduced. KB-R6933 reversed the reduction of gastric emptying induced by cisplatin. These results suggest that KB-R6933 is an antiemetic agent, and could improve the cisplatin-induced delay of gastric emptying. (C) 1999 Elsevier Science Inc. All rights reserved.

引用

页码：283 / 288

页数：6

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