Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential.

Mirko Tomić, Marija Kundaković, Biljana Butorović, Branka Janać, Deana Andrić, Goran Roglić, Djurdjica Ignjatović, Sladjana Kostić-Rajacić

Department of Biochemistry, Institute for Biological Research, 29 novembra 142, 11060 Belgrade, Serbia and Montenegro. mitomic@ibiss.bg.ac.yu

Bioorganic & medicinal chemistry letters 2004 Aug 16

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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-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 alpha 1 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.

Citation

Mirko Tomić, Marija Kundaković, Biljana Butorović, Branka Janać, Deana Andrić, Goran Roglić, Djurdjica Ignjatović, Sladjana Kostić-Rajacić. Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. Bioorganic & medicinal chemistry letters. 2004 Aug 16;14(16):4263-6