Two new phenylpiperazines with atypical antipsychotic potential.

作者: Mirko Tomić , Djurdjica Ignjatović , Gordana Tovilović , Deana Andrić , Goran Roglić

DOI: 10.1016/J.BMCL.2007.08.066

关键词: PharmacologyDopamine receptorAdrenergic receptorBicyclic moleculeChemistry5-HT receptorLigand (biochemistry)Atypical antipsychoticStereochemistryPotencyAffinities

摘要: Abstract Two new series of substituted arylpiperazines with heterocyclic 3-propoxy-benzimidazole or 3-propoxy-benzimidazole-2-thione groups were synthesized and their in vitro binding affinities for the D 2 , 5-HT 1A 2A α 1 -adrenergic receptors determined. Among them, only two compounds phenyl aryl-constituent (8a 9a) showed /D p K i ratios proposed atypical neuroleptics. As to behavioral screening on rodents, both exhibited a non-cataleptic action rats antagonized d -amphetamine-induced hyperlocomotion mice, suggesting possible antipsychotic potency.

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