(8. beta.)-6-Methylergoline amide derivatives as serotonin antagonists: N1-substituent effects on vascular 5HT2 receptor activity

…, WL Garbrecht, G Marzoni, KR Whitten…

Index: Misner; Garbrecht; Marzoni; Whitten; Cohen Journal of Medicinal Chemistry, 1990 , vol. 33, # 2 p. 652 - 656

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Citation Number: 14

Abstract

A series of (8@)-6-methylergoliie amide derivatives was synthesized with various alkyl Substituents in the"-position in order to evaluate their effectiveness in blocking vascular 5HT2 receptors. The influence of both the N'substituent and amide derivative proved to be of great importance on binding affinities to vascular 5HT2 receptors. Within each series of amides, however, maximum affinity was achieved with an N1-isopropyl substituent (14, 18 ...

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