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谷氨酸(Glu)是脊椎动物中枢神经系统中的主要兴奋性神经递质,其受体可分为代谢型和离子型两大类。离子型受体由三种组成:AMPA受体,KA受体及NMDA受体。其中NMDA受体被认为是突触可塑性及皮质和海马神经元长时程增强效应(Long-term potentiation,LTP)的主要调控者,构成了中枢神经系统的重要功能如学习和记忆的基础。NMDA受体的过度激活在多种神经系统退行性疾病的发生和发展过程中发挥着重要作用。但是,由于非选择性NMDA受体拮抗剂的选择性较低,故在发挥明显的治疗作用的同时也发生了严重的副反应,影响了其临床应用。而NMDA受体的NR2B亚单位的分布相对较集中,选择性NR2B受体拮抗剂受到了越来越多的关注。本文就近年来NMDA受体NR2B亚单位拮抗剂在神经系统退行性疾病中的研究进展作一综述。
Glutamic acid (Glu) is the main excitatory neurotransmitter in the vertebrate central nervous system. Its receptors can be divided into metabolic and ionic categories. Ionic receptors are composed of three components: the AMPA receptor, the KA receptor and the NMDA receptor. Among them, NMDA receptors are thought to be the key regulators of synaptic plasticity and long-term potentiation (LTP) in cortical and hippocampal neurons, forming the basis of important functions of the central nervous system such as learning and memory. Overexpression of NMDA receptors plays an important role in the development and progression of a variety of neurodegenerative diseases. However, due to the low selectivity of non-selective NMDA receptor antagonists, it also plays a significant role in the treatment while also having serious side effects, affecting its clinical application. However, the distribution of NR2B subunits of NMDA receptors is relatively concentrated, and selective NR2B receptor antagonists are receiving more and more attention. This review summarizes recent progress in the research of NMDA receptor NR2B subunit antagonist in neurodegenerative diseases.