AMPA受体正向变构调节剂CX717研究进展  

CX717 as a positive allosteric modulator of α-amino-3-hydroxyl-5methyl-4-isoxazole-propionic acid receptor: research advances

作　　者：贺艺超[1,2] 肖典[1] 齐倩倩[1,2] 赵国明[1] 周辛波[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850 [2]沈阳药科大学制药工程学院,沈阳110016

出　　处：《国际药学研究杂志》2013年第3期261-264,共4页Journal of International Pharmaceutical Research

摘　　要：α-氨基-3-羟基-5-甲基-4-异噁唑丙酸(AMPA)受体是离子型谷氨酸受体的一种亚型,分布于中枢神经系统的突触后膜,介导大多数快速兴奋性神经传递。CX717是由美国Cortex制药公司研制的苯甲酰胺类AMPA受体正向调节剂,能够降低AMPA受体失活或降敏的速度从而提高突触的活性,与阿尔茨海默病、帕金森病、抑郁症和注意力缺陷多动症等疾病的治疗密切相关。本文主要综述CX717在化学结构、药代动力学、毒理学和药效学方面的研究进展。α-Amino-3-hydroxyl-5-methyl-4-isoxazole-propionic acid（AMPA） receptor,a subtype of ionotropic glutamate receptors in the postsynaptic membrane of the central nervous system（CNS）,mediates most of the fast excitatory neurotransmission.CX717 developed by Cortex Pharmaceuticals Company of the USA belongs to the benzamide series of AMPA receptor positive modulators.It can reduce the speed of AMPA receptor inactivation or desensitization,thereby enhancing synaptic activity,and is closely related to the treatment of Alzheimer＇s disease,Parkinson＇s disease,depression and attention deficit hyperactivity disorder（ADHD）.This article reviews the latest research of CX717 regarding its structure,pharmacokinetics,toxicology and pharmacodynamics.

关 键 词：AMPA受体 正向变构调节剂 CX717 

分 类 号：R96[医药卫生—药理学]