Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential

Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and alpha(1) receptors. Two compounds with benztriazole group had a 5-HT2A/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-HT2A and alpha1 receptors and a higher affinity for 5-HT1A receptors than clozapine. Also, it exhibited the noncataleptic behavioural pattern of atypical antipsychotics and antagonized d-amphetamine-induced hyperlocomotion in rats. (C) 2004 Elsevier Ltd. All rights reserved.