Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as α2/α3 subtype selective GABAA agonists for the treatment of anxiety

Simon C. Goodacre,David James Hallett,Robert W. Carling,José L. Castro,David S. Reynolds,Andrew Pike,Keith A. Wafford,Robert Newman,John R. Atack,Leslie J. Street

Bioorganic & Medicinal Chemistry Letters（2006）

引用 31|浏览18

暂无评分

摘要

Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones are high affinity GABAA agonists. Compound 16d has good oral bioavailability in rat, functional selectivity for the GABAAα2 and α3-subtypes and is anxiolytic in a conditioned animal model of anxiety with minimal sedation observed at full BZ binding site occupancy.

查看译文

关键词

Imidazo[1,2-a]pyrazin-8-ones,Imidazo[1,2-d][1,2,4]triazin-8-ones,Imidazo[2,1-f][1,2,4]triazin-8-ones,GABAA agonists,Functionally selective for GABAAα2 and α3,Anxiolytic

AI 理解论文

溯源树

样例

生成溯源树，研究论文发展脉络

Chat Paper

正在生成论文摘要