NR2B受体拮抗剂及其在缺血性脑血管病中的应用  

NR2B Receptor Antagonists and Their Application in Ischemic Cerebrovascular Diseases

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作  者:杜旭辉[1] 杨金升[1] 

机构地区:[1]兰州军区总医院神经内科,730050

出  处:《国际脑血管病杂志》2007年第10期786-789,共4页International Journal of Cerebrovascular Diseases

摘  要:脑缺血时的神经损伤与谷氨酸过度兴奋N-甲基-D-天门冬氨酸(NMDA)受体有关。由于非选择性NMDA受体拮抗剂能影响所有NMDA受体而产生不良反应,其临床应用受到很大限制,因此选择性NMDA受体在近年来受到越来越多的重视。NR2B亚单位拮抗剂主要分为哌啶衍生物、酰胺衍生物、脒衍生物、氨基喹啉衍生物等,主要代表药物有艾芬地尔、依利罗地。它们能选择性作用于NMDA受体NR2B亚单位,有望成为临床上安全有效的神经保护剂。Neuronal damage is associated with the excessive stimulation of N-Methyl-D- Aspartate (NMDA) receptors by glutamate during cerebral ischemia. Because of non-selective NMDA receptor antagonist can influence all NMDA receptors and produce adverse effects, and its clinical application has been restricted significantly, an increasing attention has been paid to the selective NMDA receptor in recent years. NR2B subunit antagonists are mainly divided into piperidine derivatives, amide derivatives, amidine derivatives, and aminoquinoline derivatives, etc. The representative drugs include ifenprodil and eliprodil, These drugs can selectively act on NMDA receptor NR2B subunit, and they are expected to become safe and effective neuroprotective agents in clinical practice.

关 键 词:NR2B受体拈抗剂 脑缺血 NR2B亚单位 

分 类 号:R743[医药卫生—神经病学与精神病学]

 

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