论文部分内容阅读
α-氨基-3-羟基-5-甲基-4-异噁唑丙酸(AMPA)受体是游离型谷氨酸受体,广泛分布于中枢神经系统,介导快速兴奋性突触传递。越来越多的证据表明,其在突触可塑性及中枢敏化中发挥重要作用,并且与神经系统疾病关系密切。过度刺激AMPA受体产生兴奋性毒性会导致神经元损伤,引发癫痫、肌萎缩侧索硬化和帕金森病等一系列神经系统疾病的发生。竞争性AMPA受体拮抗剂能够有效下调AMPA受体活性,对预防和治疗神经系统疾病意义重大。本文对竞争性AMPA受体拮抗剂的研究进展进行综述。
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor is a free glutamate receptor that is widely distributed in the central nervous system and mediates rapid excitatory synaptic transmission. More and more evidences show that it plays an important role in synaptic plasticity and central sensitization, and is closely related to nervous system diseases. Excessive stimulation of AMPA receptor excitotoxicity can lead to neuronal damage, triggering a series of nervous system diseases such as epilepsy, amyotrophic lateral sclerosis and Parkinson's disease. Competitive AMPA receptor antagonists can effectively down-regulate AMPA receptor activity and are of great importance in the prevention and treatment of neurological diseases. This review summarizes the research progress of competitive AMPA receptor antagonists.