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M胆碱受体调控的M通道——神经精神药物的新靶点
引用本文:宋明柯,胡国渊,陈红专. M胆碱受体调控的M通道——神经精神药物的新靶点[J]. 中国临床药理学与治疗学, 2006, 11(11): 1219-1224
作者姓名:宋明柯  胡国渊  陈红专
作者单位:1. 上海交通大学基础医学院药理学教研室,上海,200025
2. 中国科学院上海药物研究所新药研究国家重点实验室,上海,201203
基金项目:上海市科委资助项目;上海市高校优秀青年教师科研专项基金;上海交通大学校科研和教改项目
摘    要:M通道是广泛分布于神经系统的电压门控钾通道,20多年前就发现激活M受体可使它关闭,所以命名为M通道。M通道激活后可降低神经元的兴奋性和限制重复放电的频率,因此关闭M通道能够提高神经系统的兴奋性。M通道在许多生理功能中发挥重要作用,近年发现M通道功能异常是一些神经系统疾病的发病环节,并且M通道的阻滞剂能改善认知功能,M通道的开放剂对癫痫和慢性痛有潜在治疗价值,因此M通道已逐渐成为神经精神药物的新靶点。

关 键 词:M胆碱受体  M通道  神经元  兴奋性  药物靶点
文章编号:1009-2501(2006)11-1219-06
收稿时间:2006-04-18
修稿时间:2006-05-15

Muscarinic acetylcholine receptors-coupled M channels: a new drug target for neuropsychic diseases
SONG Ming-ke,HU Guo-yuan,CHEN Hong-zhuan. Muscarinic acetylcholine receptors-coupled M channels: a new drug target for neuropsychic diseases[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2006, 11(11): 1219-1224
Authors:SONG Ming-ke  HU Guo-yuan  CHEN Hong-zhuan
Affiliation:1.Department of Pharmacology, College of Basic Medical Sciences, Shanghai Jiaotong University, Shanghai 200025, China ; 2.tate Key Laboratory of Drug Research, Shanghai Institute of Materia Medica , Chinese Academy of Sciences, Shanghai 201203, China
Abstract:The M-channel is a voltage-gated potassium channel, distributed in nervous system, playing a key role in controlling neuronal excitability. In brain, the transmitter acetylcholine increases neural activity by inhibiting M-channel via muscarinic acetylcholine receptors. This cholinergic excitation is important for alertness, arousal, learning and memory. Mutations in M-channel genes result in epilepsy and deafness. M-channel activators are efficacious for treating epilepsy and neuropathic pain; conversely, its inhibitors are useful in improving symptoms of Alzheimer's disease. Based on recent progress and findings, the M-channel has emerged as a promising drug target for treating neuropsychic diseases.
Keywords:KCNQ
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