5-Hydroxytryptamine (5-HT3) receptor antagonists. 1. Indazole and indolizine-3-carboxylic acid derivatives

J Bermudez, CS Fake, GF Joiner…

Index: Bermudez, Jose; Fake, Charles S.; Joiner, Graham F.; Joiner, Karen A.; King, Frank D.; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 7 p. 1924 - 1929

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Citation Number: 130

Abstract

3, BRL 24682: R= tion, 1 has been shown to be a relatively weak 5-hydroxytryptamine 5- HT3 receptor antagonist. 2 We have recently correlated the 5-HT3 receptor antagonist activity with the effectiveness of high-dose metoclopramide at inhibiting emesis evoked by cytotoxic agents used in cancer~ hemotherapy.~ Antagonism of 5-HT3 receptors has also been implicated for the treatment of migraine: schizo-~ hrenia,~ and anxiety. 6