Synthesis and anorectic activity of 2H-4,6-dimethyl-2-[(4-phenylpiperazin-1-yl)methyl]-3-oxo-2,3-dihydroisothiazolo[5,4-b]pyridine

被引：0
|
作者：
Malinka, W
Rutkowska, M
机构：
[1] Wroclaw B Beirut Univ, Dept Chem Drugs, PL-50137 Wroclaw, Poland
[2] Wroclaw Univ Med, Dept Pharmacol, PL-50368 Wroclaw, Poland
来源：
FARMACO | 1997年 / 52卷 / 10期
关键词：
D O I：
暂无
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The synthesis of 2H-4, 6-dimethyl-2-[(4-phenylpiperazin-1-yl)methyl]-3-oxo-2,3-dihydro-isothiazolo[5,4-b]pyridine (3) and its biological properties are described. Compound 3 pharmacologically evaluated in vivo by use of behavioral tests showed to have a profile of activity characteristic of stimulation of the central serotoninergic system, mostly 5-HT2A receptors (anorectic action: 2 mg/kg ip, 8.5 mg/kg po) However, receptor activity of isothiazolopyridine 3 was not confirmed in vitro using 5-HT2A and 5-HT1A, receptor binding technique. Molecular modeling studies demonstrated that it is difficult to predict bioactive conformation of title molecule 3.
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收藏
页码：595 / 601
页数：7
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