中国药理学通报2018，Vol.34Issue(3)：297-303,7.DOI:10.3969/j.issn.1001-1978.2018.03.001
手性抗抑郁药物评价体系的建立与应用
System for chiral antidepressant evaluation and related application
摘要
Abstract
Currently, most commercially available antidepres-sants have one or more chiral centers,and development of chiral antidepressants are of great interest for researchers. Thalidomide induced tragedy promotes drug evaluation centers from various countries to reevaluate their current guidelines and recommend single enantiomer application when developing a chiral antide-pressant. Unfortunately,as far to our knowledge,traditional en-antiomers comparison and active enantiomer selection are real-ized by simple comparison using in vitro targets data. Our team established an integrated system for chiral antidepressant evalua-tion and active enantiomer screening based on four modules,in-cluding pharmacodynamic comparison,pharmacokinetic compar-ison, toxicological comparison, and comprehensive factors. Here,we review this integrated system and make a detailed a-nalysis taking ammoxetine as a realistic example.关键词
抗抑郁药物/手性药物/评价体系/对映体/立体选择性/阿姆西汀Key words
antidepressants/chiral agents/integrated evaluation system/enantiomer/stereoselectivity/ammoxetine.分类
医药卫生引用本文复制引用
薛瑞,李云峰,张有志..手性抗抑郁药物评价体系的建立与应用[J].中国药理学通报,2018,34(3):297-303,7.基金项目
国家科技重大专项新药创制专项(No 2017ZX09309020) （No 2017ZX09309020）
国家自然科学基金面上项目( No 81274117,81302761) （ No 81274117,81302761）
