国际药学研究杂志
國際藥學研究雜誌
국제약학연구잡지
INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH
2014年
4期
407-412
,共6页
肖典%王凌霄%周辛波%李松
肖典%王凌霄%週辛波%李鬆
초전%왕릉소%주신파%리송
α-氨基-3-羟基-5-甲基-4-异唑恶唑丙酸受体%竞争性拮抗剂%中枢神经系统%受体选择性
α-氨基-3-羥基-5-甲基-4-異唑噁唑丙痠受體%競爭性拮抗劑%中樞神經繫統%受體選擇性
α-안기-3-간기-5-갑기-4-이서악서병산수체%경쟁성길항제%중추신경계통%수체선택성
α-amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid%receptor%competitive antagonists%central nervous system
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-氨基-3-羥基-5-甲基-4-異唑噁唑丙痠(AMPA)受體是遊離型穀氨痠受體,廣汎分佈于中樞神經繫統,介導快速興奮性突觸傳遞。越來越多的證據錶明,其在突觸可塑性及中樞敏化中髮揮重要作用,併且與神經繫統疾病關繫密切。過度刺激AMPA受體產生興奮性毒性會導緻神經元損傷,引髮癲癇、肌萎縮側索硬化和帕金森病等一繫列神經繫統疾病的髮生。競爭性AMPA受體拮抗劑能夠有效下調AMPA受體活性,對預防和治療神經繫統疾病意義重大。本文對競爭性AMPA受體拮抗劑的研究進展進行綜述。
α-안기-3-간기-5-갑기-4-이서악서병산(AMPA)수체시유리형곡안산수체,엄범분포우중추신경계통,개도쾌속흥강성돌촉전체。월래월다적증거표명,기재돌촉가소성급중추민화중발휘중요작용,병차여신경계통질병관계밀절。과도자격AMPA수체산생흥강성독성회도치신경원손상,인발전간、기위축측색경화화파금삼병등일계렬신경계통질병적발생。경쟁성AMPA수체길항제능구유효하조AMPA수체활성,대예방화치료신경계통질병의의중대。본문대경쟁성AMPA수체길항제적연구진전진행종술。
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.