Nonpeptide Arginine Vasopressin Antagonists for Both V1A and V2 Receptors: Synthesis and Pharmacological Properties of 2-Phenyl-4'-((2, 3, 4, 5-tetrahydro-1H-1- …

A Matsuhisa, A Tanaka, K Kikuchi, Y SHIMADA…

Index: Matsuhisa, Akira; Tanaka, Akihiro; Kikuchi, Kazumi; Shimada, Yoshiaki; Yatsu, Takeyuki; Yanagisawa, Isao Chemical and Pharmaceutical Bulletin, 1997 , vol. 45, # 11 p. 1870 - 1874

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Citation Number: 20

Abstract

A series of compounds structurally relate to 4'-[(2, 3, 4, 5-tetrahydro-1H-1-benzazepin-1-yl) carbonyl] benzanilide was synthesized and demonstrated to have arginine vasopressin (AVP) antagonist activity for both V 1A and V 2 receptors. The introduction of a phenyl or a 4- substituted phenyl group into the ortho position of the benzoyl moiety resulted in an increase in both binding affinity and antagonistic activity. The 2-(4-methylphenyl) derivative (1g) ...