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ID: ALA1137522

Journal: Bioorg Med Chem Lett

Title: Two new phenylpiperazines with atypical antipsychotic potential.

Authors: Tomić M, Ignjatović D, Tovilović G, Andrić D, Roglić G, Kostić-Rajacić S.

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), 5-HT(2A), and alpha(1)-adrenergic receptors determined. Among them, only two compounds with phenyl aryl-constituent (8a and 9a) showed 5-HT(2A)/D(2) pK(i) binding ratios proposed for atypical neuroleptics. As to their behavioral screening on rodents, both compounds exhibited a non-cataleptic action in rats and antagonized D-amphetamine-induced hyperlocomotion in mice, suggesting their possible atypical antipsychotic potency.

CiteXplore: 17870534

DOI: 10.1016/j.bmcl.2007.08.066