Polycyclic aryl-and heteroarylpiperazinyl imides as 5-HT1A receptor ligands and potential anxiolytic agents: synthesis and structure-activity relationship studies

M Abou-Gharbia, UR Patel, MB Webb…

Index: Abou-Gharbia, Magid; Patel, Usha R.; Webb, Michael B.; Moyer, John A.; Andree, Terrance H.; Muth, Eric A. Journal of Medicinal Chemistry, 1988 , vol. 31, # 7 p. 1382 - 1392

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Citation Number: 49

Abstract

A series of polycyclic aryl-and heteroarylpiperazinyl imides were prepared and tested in various receptor-binding and behavioral tests. Parameters measured included in vitro inhibition of Dz and 5-HTlA receptor binding, inhibition of apomorphine (APO) induced stereotyped and climbing behavior, and activity in blocking conditioned avoidance responding (CAR). Several compounds demonstrated moderate to high affinity for the 5- ...