Two new phenylpiperazines with atypical antipsychotic potential

被引：24
|
作者：
Tomic, Mirko
Ignjatovic, Djurdjica
Tovijovic, Gordana
Andric, Deana
Roglic, Goran
Kostic-Rajacic, Sladjana
机构：
[1] Inst Biol Res, Dept Biochem, Belgrade 11060, Serbia
[2] Fac Chem, Belgrade 11000, Serbia
[3] Inst Chem Technol & Met, Belgrade 11000, Serbia
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 21期
关键词：
arylpiperazines; dopamine receptors; serotonin receptors; atypical antipsychotics; RECEPTOR; ROXINDOLE; DRUG;
D O I：
10.1016/j.bmcl.2007.08.066
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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,, 5-HT1A, 5-HT2A, and alpha-adrenergic receptors determined. Among them, only two compounds with phenyl aryl-constituent (8a and 9a) showed 5-HT2A/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. (c) 2007 Elsevier Ltd. All rights reserved.
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页码：5749 / 5753
页数：5
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