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3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.

Abstract：

:A novel series of 3-heteroaryl-5,6-bis(aryl)-1-methyl-2-pyridones were developed with high affinity for the benzodiazepine (BZ) binding site of human gamma-aminobutyric acid (GABA(A)) receptor ion channels, low binding selectivity for alpha 2- and/or alpha 3- over alpha 1-containing GABA(A) receptor subtypes and high binding selectivity over alpha 5 subtypes. High affinity appeared to be associated with a coplanar conformation of the pyridone and sulfur-containing 3-heteroaryl rings resulting from an attractive S.O intramolecular interaction. Functional selectivity (i.e., selective efficacy) for alpha 2 and/or alpha 3 GABA(A) receptor subtypes over alpha1 was observed in several of these compounds in electrophysiological assays. Furthermore, an alpha 3 subtype selective inverse agonist was proconvulsant and anxiogenic in rodents while an alpha 2/alpha 3 subtype selective partial agonist was anticonvulsant and anxiolytic, supporting the hypothesis that subtype selective BZ site agonists may provide new anxiolytic therapies.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Collins I,Moyes C,Davey WB,Rowley M,Bromidge FA,Quirk K,Atack JR,McKernan RM,Thompson SA,Wafford K,Dawson GR,Pike A,Sohal B,Tsou NN,Ball RG,Castro JL

doi

10.1021/jm0110789

keywords:

subject

Has Abstract

pub_date

2002-04-25 00:00:00

pages

1887-900

issue

9

eissn

0022-2623

issn

1520-4804

pii

jm0110789

journal_volume

45

pub_type

杂志文章

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