Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and α₁ receptors. Two compounds with benztriazole group had a 5-HT_2A/D₂ 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 D₂, 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.