新型多巴胺D_2类受体部分激动剂brexpiprazole  

A novel dopamine D_2 receptor partial agonist: brexpiprazole

作　　者：刘长鹰[1] 于鹏[2] 李祎亮[1] 

机构地区：[1]天津药物研究院天津市新药设计与发现重点实验室,天津300193 [2]天津药物研究院医药信息中心,天津300193

出　　处：《现代药物与临床》2014年第2期196-200,共5页Drugs & Clinic

摘　　要：在多巴胺D2类受体中,D2受体部分激动剂对中脑边缘通路可产生功能性拮抗作用,能有效的改善精神分裂症因D2过度活动引起的阳性症状;对中脑皮层通路可产生功能性激动作用,可改善D2功能低下所引起的阴性症状、认知损害。brexpiprazole是一种新型多靶点作用机制的用于精神障碍疾病的治疗药物,除主要具备多巴胺D2受体部分激动作用之外,还具备D3受体部分激动作用、5-HT1A部分受体激动作用和5-HT2A部分受体拮抗作用,是针对单胺类神经递质多靶点开发的同时具有抗精神分裂和抗抑郁作用的新药,目前正在进行Ⅲ期临床试验。Among the dopamine receptors, dopamine D2 receptor partial agonist can cause the functional antagonism to mesolimbic pathway and effectively improve the positive symptom caused by overactive D2 receptor in schizophrenia. While it can cause functional activation to mesocortical pathway and effectively improve the negative symptom and cognitive impairment caused by depressed D2 receptor function in schizophrenia. Brexpiprazole is a medicine with novel multi-target effect mechanism for the treatment in mental disorders. Besides main dopamine D2 receptor partial activation, brexpiprazole has dopamine D3 receptor partial activation, 5-HTIA receptor partial activation, and 5-HT2A receptor partial antagonism. It is a novel medicine with the anti-schizophrenia and anti-depression effect developed in aiming at multi-targets of monoamine neurotransmitter and now is undergoing phase III chinical trial.

关 键 词：brexpiprazole 多巴胺D2类受体部分激动剂 精神分裂 抑郁 

分 类 号：R917[医药卫生—药物分析学]