Novel Pyrrolo[1,2-a]Pyrazines (TSPO Ligands) with Anxiolytic Activity Dependent on Neurosteroid Biosynthesis

被引：0
作者：
M. A. Yarkova
G. V. Mokrov
T. A. Gudasheva
S. B. Seredenin
机构：
[1] Russian Academy of Medical Sciences,Zakusov State Institute of Pharmacology
来源：
Pharmaceutical Chemistry Journal | 2016年 / 50卷
关键词：
18 kDa translocator protein; anxiolytic activity; pyrrolo[1,2-; ]pyrazines; neurosteroids;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A series of novel pyrrolo[1,2-a]pyrazines that were ligands of 18 kDa translocator protein (TSPO) were synthesized at Zakusov SIP. The compounds N-benzyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-1) and N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3) were found to possess high TSPO affinity and pronounced anxiolytic activity. The anxiolytic effects of GML-1 and GML-3 in elevated plus-maze tests were completely blocked by the neurosteroidogenic-enzyme inhibitors trilostane and finasteride.
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页码：501 / 504
页数：3
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