以突触囊泡蛋白2A(SV2A)为靶点的抗癫痫药物研究进展  

Advances in antiepileptic drugs targeting synaptic vesicular protein 2A(SV2A)

作　　者：张宁 张宗磊 陈明 毋立华 蔡文卿 ZHANG Ning;ZHANG Zonglei;CHEN Ming;WU Lihua;CAI Wenqing(Key Laboratory for Chemical Drug Research of Shandong Province,Shandong Academy of Pharmaceutical Sciences,Jinan 250000,China;Shandong Center for Food and Drug Evaluation&Inspection,Jinan 250000,China)

机构地区：[1]山东省药学科学院山东省生物药物重点实验室,山东济南250000 [2]山东省食品药品审评查验中心,山东济南250000

出　　处：《沈阳药科大学学报》2024年第4期526-536,共11页Journal of Shenyang Pharmaceutical University

摘　　要：抗癫痫药物是癫痫患者的首选治疗癫痫手段。全球癫痫发病率的不断提高,给国家、个人和家庭生活等带来较大经济负担。随着越来越多的癫痫患者得到规范化治疗,使得抗癫痫药物临床需求越来越大。突触囊泡蛋白2A(synaptic vesicle protein 2A,SV2A)通过调节神经递质的释放,来维持脑内兴奋性神经递质和抑制性神经递质的平衡。随着SV2A确证为新的抗癫痫靶点,左乙拉西坦和布瓦西坦的上市,抗癫痫靶点和抗癫痫新药进一步丰富。本文围绕抗癫痫药物靶点SV2A以及以SV2A为靶点的上市及在研药物做概述,并对其构效关系进行总结。Antiepileptic drugs are the first choice of treatment for epilepsy patients.The incidence of epilepsy is increasing all over the world,which brings great burden to national economy and personal life.As more and more epilepsy patients get standardized treatment,there is a growing clinical demand for antiepileptic drugs.Synaptic vesicle protein 2A(SV2A)maintains a balance between excitatory and inhibitory neurotransmitters in the brain by regulating neurotransmitter release.With the confirmation of new antiepileptic target SV2A and the marketing of levetiracetam and brivaracetam,antiepileptic targets and new antiepileptic drugs are further enriched.In this paper,the target SV2A and the drugs marketed and under development targeting SV2A were summarized,and their structure-activity relationship was summarized.

关 键 词：癫痫 SV2A 左乙拉西坦 布瓦西坦 构效关系 

分 类 号：R914[医药卫生—药物化学]