N-(indol-3-ylglyoxylyl)piperidines:: High affinity agonists of human GABA-A receptors containing the α1 subunit

被引：11

作者：

Collins, I

Davey, WB

Rowley, M

Quirk, K

Bromidge, FA

McKernan, RM

Thompson, SA

Wafford, KA

机构：

[1] Merck Sharp & Dohme Res Labs, Dept Med Chem, Neurosci Res Ctr, Harlow CM20 2QR, Essex, England

[2] Merck Sharp & Dohme Res Labs, Dept Biochem, Neurosci Res Ctr, Harlow CM20 2QR, Essex, England

[3] Merck Sharp & Dohme Res Labs, Dept Pharmacol, Neurosci Res Ctr, Harlow CM20 2QR, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(00)00245-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new class of N-(indol-3-ylglyoxylyl)piperidines are high affinity agonists at the benzodiazepine binding site of human GABA-A receptor ion-channels, with modest selectivity for receptors containing the alpha(1) subunit over alpha(2) and alpha(3). All three receptor subtypes discriminate substantially between the two enantiomers of the chiral ligand 10. (C) 2000 Elsevier Science Ltd. All rights reserved.

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页码：1381 / 1384

页数：4

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