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α-氨基羟甲基唑丙酸(AMPA)受体广泛分布于具有兴奋性的神经突触中,在中枢神经系统中起着重要作用,神经退行性障碍、行动障碍、精神疾病、疼痛等许多疾病都涉及到AMPA受体。日本Eisai公司的在研新药Perampanel(E2007)作为首个具有高度选择性和非竞争性的AMPA型谷氨酸盐受体拮抗剂,用于治疗难治性癫痫的部分发作。基于3个Ⅲ期临床试验具有良好结果,2011年该公司已向美国和欧洲提交了该药物的营销许可申请。
Alpha-amino hydroxymethyl pyrazole propionate (AMPA) receptors are widely distributed in excitatory neuronal synapses and play an important role in the central nervous system. Many neurodegenerative disorders, mobility disorders, mental disorders, pain, and the like Diseases all involve AMPA receptors. As the first highly selective and noncompetitive AMPA glutamate receptor antagonist at Japan’s Eisai’s investigational new drug Perampanel (E2007), it is used to treat partial seizures of refractory epilepsy. Based on the good results of three Phase III clinical trials, the company submitted its marketing approval application for the drug to the United States and Europe in 2011.