Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines

…, A Gobert, S Le Marouille-Girardon…

Index: Peglion; Canton; Bervoets; Audinot; Brocco; Gobert; Le Marouille-Girardon; Millan Journal of Medicinal Chemistry, 1995 , vol. 38, # 20 p. 4044 - 4055

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Citation Number: 38

Abstract

Benzocycloalkyl and benzocycloalkenyl moities linked, directly or via an alkyl chain, to oxygenbearing heteroarylpiperazines were synthesized, in an attempt to obtain potent and selective antagonists at postsynaptic 5-HT1. 4 receptors. From the numerous arylpiperazines described in the literature, 1-(2, 3-dihydro-1, 4-benzodioxin-5-yl) piperazine (3a) was chosen as a model of an arylpiperazine in view of its selectivity for 5-HT1. 4 ...