Young A B, Fagg G E
Department of Neurology, University of Michigan, Ann Arbor 48104.
Trends Pharmacol Sci. 1990 Mar;11(3):126-33. doi: 10.1016/0165-6147(90)90199-i.
In last month's article in this series, Lodge and Johnson discussed the contribution of noncompetitive excitatory amino acid antagonists to understanding of these receptors. In this third article, Anne Young and Graham Fagg describe how radioligand binding experiments have helped to fuel the recent burst of progress in understanding excitatory amino acid receptors in the brain. New and selective radioligands have facilitated mapping the distributions of the major excitatory receptor subtypes in normal and diseased brain, examining allosteric interactions within the NMDA receptor, searching for novel therapeutic agents and determining drug mechanisms, and making first steps along the path to defining receptor structure at the molecular level.
在上个月本系列的文章中，洛奇和约翰逊讨论了非竞争性兴奋性氨基酸拮抗剂对理解这些受体的贡献。在这第三篇文章中，安妮·杨和格雷厄姆·法格描述了放射性配体结合实验如何助力推动了近期在理解大脑中兴奋性氨基酸受体方面取得的一系列进展。新型选择性放射性配体有助于绘制正常和患病大脑中主要兴奋性受体亚型的分布图，研究NMDA受体内部的变构相互作用，寻找新型治疗药物并确定药物作用机制，以及在分子水平上定义受体结构的道路上迈出第一步。
