A mutation in the glycine binding pocket of the N-methyl-D-aspartate receptor NR1 subunit alters agonist efficacy

被引：8

作者：

Wood, MW ^{[1
]}

VanDongen, HMA ^{[1
]}

VanDongen, AMJ ^{[1
]}

机构：

[1] Duke Univ, Med Ctr, Dept Pharmacol & Canc Biol, Durham, NC 27710 USA

来源：

MOLECULAR BRAIN RESEARCH | 1999年 / 73卷 / 1-2期

关键词：

NMDA receptor; pharmacology; efficacy; affinity; DCK; HA-966;

D O I：

10.1016/S0169-328X(99)00247-8

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

Alanine 714 of the NMDA receptor NR1 subunit resides in the glycine binding pocket. The Ala714Leu mutation substantially shifts glycine affinity, but here no effect on antagonism by DCK is detected. Ala714Leu is also found to limit the efficacy of a partial agonist without altering its apparent affinity. The differential sensitivity of Ala714Leu to glycine agonists suggests that alanine 714 may be an intermediary in transducing the ligand binding signal. (C) 1999 Elsevier Science B.V. All rights reserved.

引用

页码：189 / 192

页数：4

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