2,5-dihydropyrazolo[4,3-c]pyridin-3-ones:: functionally selective benzodiazepine binding site ligands on the GABAA receptor

被引:22
作者
Mitchinson, A [1 ]
Atack, JR [1 ]
Blurton, P [1 ]
Carling, RW [1 ]
Castro, JL [1 ]
Curley, KS [1 ]
Russell, MGN [1 ]
Marshall, G [1 ]
McKernan, RM [1 ]
Moore, KW [1 ]
Narquizian, R [1 ]
Smith, A [1 ]
Street, LJ [1 ]
Thompson, SA [1 ]
Wafford, K [1 ]
机构
[1] Merck Sharp & Dohme Res Labs, Ctr Res Neurosci, Harlow CM20 2QR, Essex, England
关键词
D O I
10.1016/j.bmcl.2004.04.085
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones are GABA(A) receptor benzodiazepine binding site ligands with functional selectivity for the alpha(3) subtype over the alpha(1) subtype. SAR studies to optimise this functional selectivity are described. (C) 2004 Published by Elsevier Ltd.
引用
收藏
页码:3441 / 3444
页数:4
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