Synthesis, Structure-Activity Relationships, and Biological Properties of 1-Heteroaryl-4-[ω-(1 H-indol-3-yl) alkyl] piperazines, Novel Potential Antipsychotics Combining …

…, R van Hes, JP de Moes, AP den Hartog…

Index: Smid, Pieter; Coolen, Hein K. A. C.; Keizer, Hiskias G.; Van Hes, Rolf; De Moes, Jan-Peter; Den Hartog, Arnold P.; Stork, Bob; Plekkenpol, Rob H.; Niemann, Leonarda C.; Stroomer, Cees N. J.; Tulp, Martin Th. M.; Van Stuivenberg, Herman H.; McCreary, Andrew C.; Hesselink, Mayke B.; Herremans, Arnoud H. J.; Kruse, Chris G. Journal of Medicinal Chemistry, 2005 , vol. 48, # 22 p. 6855 - 6869

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Citation Number: 56

Abstract

A series of novel bicyclic 1-heteroaryl-4-[ω-(1 H-indol-3-yl) alkyl] piperazines was synthesized and evaluated on binding to dopamine D2 receptors and serotonin reuptake sites. This class of compounds proved to be potent in vitro dopamine D2 receptor antagonists and in addition were highly active as serotonin reuptake inhibitors. Some key representatives showed potent pharmacological in vivo activities after oral dosing in both ...