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
收藏
页码：1645 / 1647
页数：3
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