title: Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential.
abstract: 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.
authors.affiliation: Department of Biochemistry, Institute for Biological Research, 29 novembra 142, 11060 Belgrade, Serbia and Montenegro. mitomic@ibiss.bg.ac.yu
authors.forename: Mirko
authors.initials: M
authors.lastname: Tomić
authors.forename: Marija
authors.initials: M
authors.lastname: Kundaković
authors.forename: Biljana
authors.initials: B
authors.lastname: Butorović
authors.forename: Branka
authors.initials: B
authors.lastname: Janać
authors.forename: Deana
authors.initials: D
authors.lastname: Andrić
authors.forename: Goran
authors.initials: G
authors.lastname: Roglić
authors.forename: Djurdjica
authors.initials: D
authors.lastname: Ignjatović
authors.forename: Sladjana
authors.initials: S
authors.lastname: Kostić-Rajacić
mesh_terms: D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology*; D001522:Behavior, Animal; D010879:Piperazines / Q000494:pharmacology*; D051381:Rats; D011954:Receptors, Dopamine / Q000187:drug effects; D011985:Receptors, Serotonin / Q000187:drug effects
chemical_list: D014150:Antipsychotic Agents; D010879:Piperazines; D011954:Receptors, Dopamine; D011985:Receptors, Serotonin