System for chiral antidepressant evaluation and related application
10.3969/j.issn.1001-1978.2018.03.001
- VernacularTitle:手性抗抑郁药物评价体系的建立与应用
- Author:
Rui XUE
1
;
Yun-Feng LI
;
You-Zhi ZHANG
Author Information
1. 军事医学研究院毒物药物研究所
- Keywords:
antidepressants;
chiral agents;
integrated evaluation system;
enantiomer;
stereoselectivity;
ammoxetine.
- From:
Chinese Pharmacological Bulletin
2018;34(3):297-303
- CountryChina
- Language:Chinese
-
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.
