Antagonists and agonists at the glycine site of the NMDA receptor for therapeutic interventions

被引:59
作者
Jansen, M [1 ]
Dannhardt, G [1 ]
机构
[1] Johannes Gutenberg Univ Mainz, Inst Pharm, Dept Med & Pharmaceut Chem, D-55099 Mainz, Germany
关键词
glycine site; NMDA receptor; excitatory amino acid receptor; stroke; epilepsy; dementia; pain; schizophrenia;
D O I
10.1016/S0223-5234(03)00113-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
For decades neuroreceptor research has focused on the development of NMDA glycine-site antagonists, after Johnson and Ascher found out in 1987 about the co-agonistic character of this achiral amino acid at the NMDA receptor. Contrary to the inhibitory glycine receptor (glycine(A)) the glycine binding site on the NMDA receptor (glycine(B)) is strychnine-insensitive. A great diversity of diseases showing a disturbed glutamate neurotransmission have been linked to the NMDA receptor. Glycine site antagonists have been investigated for acute diseases like stroke and head trauma as well as chronic ones like dementia and chronic pain. (C) 2003 Editions scientifiques et medicales Elsevier SAS. All rights reserved.
引用
收藏
页码:661 / 670
页数:10
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