摘要
α4β2型烟碱受体(nAChR)是一种配体门控离子通道,在整个神经系统几乎都有分布,参与乙酰胆碱、多巴胺、γ-氨基丁酸、去甲肾上腺素等神经递质的调节和释放,在机体的学习、记忆、认知、注意力、炎症以及疼痛中发挥重要作用。大量研究表明,α4β2型nAChR是阿尔茨海默症、帕金森病、癫痫、抑郁症、尼古丁依赖、疼痛等神经系统性疾病的重要治疗靶点,对以老年痴呆为主的神经退行性疾病早期诊断和疗效检测具有重要意义。本文总结了α4β2型nAChR在神经系统性疾病治疗中的作用、机制以及相关药物研究进展,为筛选和开发更合适的α4β2型nAChR相关化合物提供理论依据。
Theα4β2-nicotinic acetylcholine receptor(nAChR)is a ligand-gated ion channel that is distributed throughout the nervous system.It is involved in the regulation of various neurotransmitters including acetylcholine,dopamine,γ-aminobutyric acid,and norepinephrine.α4β2-nAChR plays an important role in learning,memory,cognition,attention,inflammation,and pain.A large number of studies have shown thatα4β2-nAChR is an important therapeutic target for neurological diseases such as Alzheimer's disease,Parkinson's disease,epilepsy,depression,nicotine dependence,pain,etc.It is an important target in the early diagnosis and curative effect detection of neurodegenerative diseases including Alzheimer's disease.This review summarizes the role,mechanisms and related drug research advances onα4β2-nAChR ligand drugs in neurological diseases,as well as providing a theoretical basis for identifying and developing more suitableα4β2-nAChR-related compounds.
作者
孔德文
于子茹
周启蒙
杜冠华
KONG De-wen;YU Zi-ru;ZHOU Qi-meng;DU Guan-hua(Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China)
出处
《药学学报》
CAS
CSCD
北大核心
2021年第1期1-8,共8页
Acta Pharmaceutica Sinica
基金
中国医学科学院医学与健康科技创新工程资助项目(2017-I2M-1-010)
国家自然科学基金资助项目(81603100).