Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships

…, WB Lacefield, W Bloomquist, W Pfeifer…

Index: Robertson, David W.; Lacefield, William B.; Bloomquist, William; Pfeifer, William; Simon, Richard L.; Cohen, Marlene L. Journal of Medicinal Chemistry, 1992 , vol. 35, # 2 p. 310 - 319

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Citation Number: 42

Abstract

Antagonists of 5HT3 receptors are clinically effective in treating nausea and emesis associated with certain oncolytic drugs, including cisplatin. Moreover, these agents may be useful in pharmacological management of several central nervous system disorders, including anxiety, schizophrenia, dementia, and substance abuse. Our studies on aroyltropanamides led to the discovery that dihydrobenzofuranyl esters and amides are ...