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-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.
Mesh Terms:
Animals, Antipsychotic Agents, Behavior, Animal, Piperazines, Rats, Receptors, Dopamine, Receptors, Serotonin
Bioorg. Med. Chem. Lett.
Date: Aug. 16, 2004
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