Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential

Abstract

Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and α 1 receptors. Two compounds with benztriazole group had a 5-HT 2A /D 2 binding ratio characteristic for atypical neuroleptics (>1, pK i values). Compound 2, 5-{2-[4-(2,3-dimethyl-phenyl)-piperazin-1-yl]ethyl}1H-benzotriazole, expressed clozapine-like in vitro binding profile at D 2 , 5-HT 2A and α1 receptors and a higher affinity for 5-HT 1A receptors than clozapine. Also, it exhibited the noncataleptic behavioural pattern of atypical antipsychotics and antagonized d-amphetamine-induced hyperlocomotion in rats. © 2004 Elsevier Ltd. All rights reserved.