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 α1 receptors. Two compounds with benztriazole group had a 5-HT2A/D2 binding ratio characteristic for atypical neuroleptics (>1, pKi 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-HT2A and α1 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.