Two new phenylpiperazines with atypical antipsychotic potential.
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.
Tomić
Mirko
M
Department of Biochemistry, Institute for Biological Research, Bul. Despota Stefana 142, 11060 Belgrade, Serbia. mitomic@ibiss.bg.ac.yu
Ignjatović
Djurdjica
D
Tovilović
Gordana
G
Andrić
Deana
D
Roglić
Goran
G
Kostić-Rajacić
Sladjana
S
D000818:Animals; D014150:Antipsychotic Agents / Q000737:chemistry / Q000494:pharmacology*; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats
D014150:Antipsychotic Agents; D010879:Piperazines; C031503:phenylpiperazine