Imidazo[1,2-B][1,2,4]Triazines As Alpha 2/Alpha 3 Subtype Selective Gaba(A) Agonists For The Treatment Of Anxiety

Asr Jennings,Rt Lewis,Mgn Russell,Dj Hallett,Lj Street,Jl Castro, Jr Atack,Sm Cook, R Lincoln,J Stanley,Aj Smith,Ds Reynolds,B Sohal, A Pike,Gr Marshall,Ka Wafford, Wfa Sheppard, Sj 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 GABA(A) receptors that are functionally selective for the alpha 2/alpha 3 subtypes over the alpha 1 subtype. SAR studies to optimise this functional selectivity, pharmacokinetic and behavioural data are described. (C) 2006 Elsevier Ltd. All rights reserved.

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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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