4-CARBOXY-3-HYDROXYPHENYLGLYCINE, AN ANTAGONIST AT TYPE-I METABOTROPIC GLUTAMATE RECEPTORS

被引：18

作者：

THOMSEN, C

SUZDAK, PD

机构：

[1] Department of Receptor Neurochemistry, Pharmaceuticals Division, Novo Nordisk A/S, DK-2760 Måløv, Novo Nordisk Park

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION | 1993年 / 245卷 / 03期

关键词：

METABOTROPIC GLUTAMATE RECEPTORS; 4-CARBOXY-3-HYDROXYPHENYLGLYCINE; (1S,3R)-1-AMINOCYCLOPENTANE-1,3-DICARBOXYLATE (T-ACPD);

D O I：

10.1016/0922-4106(93)90112-M

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The pharmacology of (DL)-4-carboxy-3-hydroxyphenylglycine was examined in baby hamster kidney cells which stably express the type I metabotropic glutamate receptor (mGluR1alpha). DL-4-Carboxy-3-hydroxyphenylglycine dose-dependently inhibited glutamate-stimulated phosphoinositide hydrolysis in a competitive manner with a K(B) of 29 muM as estimated from Schild-plot analysis. The present report is the first demonstration of a potent and competitive antagonist of the mGluR1alpha subtype.

引用

页码：299 / 301

页数：3

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