Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1α metabotropic glutamate receptor

被引：47

作者：

Hermans, E ^{[1
]}

Nahorski, SR ^{[1
]}

Challiss, RAJ ^{[1
]}

机构：

[1] Univ Leicester, Dept Cell Physiol & Pharmacol, Leicester LE1 9HN, Leics, England

来源：

NEUROPHARMACOLOGY | 1998年 / 37卷 / 12期

基金：

英国惠康基金;

关键词：

glutamate; mGlu1 alpha receptor; phosphoinositide hydrolysis; non-competitive antagonist; CPCCOEt;

D O I：

10.1016/S0028-3908(98)00132-4

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

In transfected CHO cells expressing the human metabotropic glutamate receptor mGlu1 alpha, 7- hydroxyimino)cyclopropan[b]chromen-1a-carboxylic acid ethylester (CPCCOEt) was found to antagonize L-quisqualate-induced phosphoinositide hydrolysis in a non-competitive and reversible manner (apparent pK(i) value, 4.76 +/- 0.18: It = 3. This suggests that CPCCOEt antagonizes type Ir metabotropic glutamate receptor activation by interacting with a site distinct from the agonist binding site. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1645 / 1647

页数：3

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