Kemp J A, Leeson P D
Department of Pharmacology, Merck Sharp & Dohme Research Laboratories, Harlow, Essex, UK.
Trends Pharmacol Sci. 1993 Jan;14(1):20-5. doi: 10.1016/0165-6147(93)90108-v.
The glycine site on the NMDA receptor complex has generated an enormous amount of interest since it was first described five years ago. In this review by John Kemp and Paul Leeson the structure-activity relationships of agonists, partial agonists and antagonists acting at the glycine site are reviewed, along with what has been learned from studies with these compounds about the role of this site in physiological and pathological processes. Studies with prototype antagonists, and low-efficacy partial agonists that penetrate the brain, show that these compounds possess anticonvulsant and neuroprotective properties but lack some of the side-effects of other types of NMDA antagonists.
自五年前首次被描述以来，N-甲基-D-天冬氨酸（NMDA）受体复合物上的甘氨酸位点引发了极大的关注。在约翰·肯普（John Kemp）和保罗·利森（Paul Leeson）撰写的这篇综述中，对作用于甘氨酸位点的激动剂、部分激动剂和拮抗剂的构效关系进行了综述，同时也介绍了从这些化合物的研究中所了解到的该位点在生理和病理过程中的作用。对原型拮抗剂以及能够穿透大脑的低效部分激动剂的研究表明，这些化合物具有抗惊厥和神经保护特性，但没有其他类型NMDA拮抗剂的一些副作用。
