选择性mGluR1拮抗剂的研究进展  

Research progress of selective mGluR1 antagonists

作　　者：杨依磊[1] 孙薇[1] 彭诚[1] 张晓叶[1] 杨晓虹[1] 

机构地区：[1]吉林大学药学院药物化学教研室,吉林长春130021

出　　处：《药学学报》2011年第10期1167-1172,共6页Acta Pharmaceutica Sinica

摘　　要：代谢型谷氨酸受体1(mGluR1)作为代谢型谷氨酸受体的重要成员之一,在中枢神经系统的信号传导中起着重要作用。选择性mGluR1拮抗剂可以阻断mGluR1介导的信号通路,发挥镇痛、抗焦虑、抗抑郁等一系列生理功能。目前,选择性mGluR1拮抗剂的发现和优化成为人们研究的热点。本文对近10年选择性mGluR1拮抗剂的各类结构和构效关系进行综述。As an important member of metabotropic glutamate receptors（mGluR）,metabotropic glutamate receptor 1（mGluR1） plays an important role in the signal transduction of central nervous system.Selective mGluR1 antagonists can block the signaling pathway activated by mGluR1 and exert a series of physiological actions including analgesia,antianxiety,antidepression,etc.Currently,the discovery and modification of selective mGluR1 antagonists have become a hot research focus.This paper reviews the structural catalogs of selective mGluR1 antagonists and their structure-activity relationships in the last decade.

关 键 词：代谢型谷氨酸受体1 选择性拮抗剂 构效关系 进展 

分 类 号：R916[医药卫生—药学]