Imidazo[1,2-b][1,2,4]triazines as α2/α3 subtype selective GABAA agonists for the treatment of anxiety

Andrew S. R. Jennings,Richard T. Lewis,Michael G. N. Russell,David J. Hallett,Leslie J. Street,José L. Castro,John Atack,Susan M. Cook,Rachael J. Lincoln, John C. Stanley,Alison J. Smith,David S. Reynolds,Bindi Sohal,Andrew Pike,George R. Marshall,Keith A. Wafford, Wayne F. A. Sheppard,Spencer J. Tye

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

Imidazo[1,2-a]pyrimidines and imidazo[1,2-b][1,2,4]triazines are ligands for the benzodiazepine binding site of GABAA receptors that are functionally selective for the α2/α3 subtypes over the α1 subtype. SAR studies to optimise this functional selectivity, pharmacokinetic and behavioural data are described.

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关键词

imidazo[1,2-a]pyrimidines, imidazo[1,2-b][1,2,4]triazines, GABAA receptors, alpha 2/alpha 3 subtype selective, anxiolytic

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