[關鍵詞]
[摘要]
在多巴胺D2類受體中,D2受體部分激動劑對中腦邊緣通路可產生功能性拮抗作用,能有效的改善精神分裂癥因D2過度活動引起的陽性癥狀;對中腦皮層通路可產生功能性激動作用,可改善D2功能低下所引起的陰性癥狀、認知損害。brexpiprazole是一種新型多靶點作用機制的用于精神障礙疾病的治療藥物,除主要具備多巴胺D2受體部分激動作用之外,還具備D3受體部分激動作用、5-HT1A部分受體激動作用和5-HT2A部分受體拮抗作用,是針對單胺類神經(jīng)遞質多靶點開發(fā)的同時具有抗精神分裂和抗抑郁作用的新藥,目前正在進行Ⅲ期臨床試驗。
[Key word]
[Abstract]
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-HT1A 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.
[中圖分類號]
[基金項目]