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α-氨基-3-羟基-5-甲基-4-异唑恶唑丙酸(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。“,”α-Amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid (AMPA) receptor, a subtype of ionotropic glutamate receptors widely distributed in the central nervous system, mediates the fast excitatory neurotransmission. Meanwhile more and more evidence indicates that AMPA receptor plays an important role in synaptic plasticity as well as central sensitization, and it also has close relationships with nervous system diseases. Over stimulation of AMPA receptor would produce excitotoxicity, leading to neuronal damage and finally resulting in a multitude of nervous system diseases, such as epilepsy, amyotrophic lateral scelerosis,Parkinson′s dis-ease. Competitive AMPA receptor antagonists that downregulate AMPA receptor′s function are of great importance in the prevention and treatment of nervous system diseases. This article reviews the research advances of competitive AMPA receptor antagonists.