Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α1-adrenoceptors

…, CT Christoffersen, B Bang-Andersen…

Index: Kristensen, Jesper L.; Pueschl, Ask; Jensen, Martin; Risgaard, Rune; Christoffersen, Claus T.; Bang-Andersen, Benny; Balle, Thomas Journal of Medicinal Chemistry, 2010 , vol. 53, # 19 p. 7021 - 7034

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Citation Number: 7

Abstract

A series of 1-(10, 11-dihydrodibenzo [b, f] thiepin-10-yl)-4-methylpiperazine analogues substituted in the 8-position of the 10, 11-dihydrodibenzo [b, f] thiepine scaffold with aryl, heteroaryl, amine, and amide substituents are described. The compounds were designed using the previously reported Liljefors− Bøgesø pharmacophore model for dopamine D2 and α1-adrenoceptor antagonists, with the aim of obtaining selective α1-adrenoceptor ...