M胆碱受体调控的M通道———神经精神药物的新靶点

中国临床药理学与治疗学 ›› 2006, Vol. 11 ›› Issue (11): 1219-1224.

M胆碱受体调控的M通道———神经精神药物的新靶点

宋明柯, 胡国渊¹, 陈红专

上海交通大学基础医学院药理学教研室, 上海 200025;
¹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

收稿日期:2006-04-18 修回日期:2006-05-15 出版日期:2006-11-26 发布日期:2020-11-06
通讯作者: 陈红专,男, 博士, 教授, 博士生导师, 研究方向:神经药理学。Tel:021-64674721 　E-mail:yaoli@shsmu.edu.cn
作者简介:宋明柯, 男, 博士, 讲师, 研究方向:神经药理学。Tel:021-63846590-776449 E-mail:mksong@hotmail.com
基金资助:
上海市科委基础研究重点项目(No03JC14064); 上海高校优秀青年教师科研专项基金项目(2005); 上海交通大学基础医学院基金项目(2005)

Muscarinic acetylcholine receptors-coupled M channels:a new drug target for neuropsychic diseases

SONG Ming-ke, HU Guo-yuan¹, CHEN Hong-zhuan

Department of Pharmacology , College of Basic Medical Sciences , Shanghai Jiaotong University , Shanghai 200025 , China;
¹StateKey Laboratory of Drug Research , Shanghai Institute of MateriaMedica , Chinese Academy of Sciences , Shanghai 201203 , China

Received:2006-04-18 Revised:2006-05-15 Online:2006-11-26 Published:2020-11-06

摘要/Abstract

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, KCNQ, 神经元, 兴奋性, 药物靶点

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.

Key words: muscarinic acetylcholine receptors, Mchannel, KCNQ, neuron, excitability, drug targets

中图分类号:

R338
R964

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.

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.

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