Ketanserin analogs: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding

…, SP Ingher, M Teitler, RA Glennon

Index: Herndon, Jeff L.; Ismaiel, Abd; Ingher, Stacy P.; Teitler, M.; Glennon, Richard A. Journal of Medicinal Chemistry, 1992 , vol. 35, # 26 p. 4903 - 4910

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Citation Number: 124

Abstract

Ketanserin is the prototypic 5-HTz serotonin antagonist; although it has been an important tool for the study of serotonin pharmacology, it has had relatively little impact on drug design because remarkably little is known about its structure-affinity relationships. Furthermore, ketanserin also binds at 5-HTlc receptors and even less is known about the influence of its structural features on 5-HTlc receptor affinity. The present study reveals that the fluoro and ...