罗丹宁衍生物Lj0104在大鼠体内的代谢产物研究
In vivo metabolism of a rhodanine derivative Lj0104 in rats
陈晶磊 1汪维鹏 1孙伟振 1李静 1乔春华1
作者信息
- 1. 苏州大学医学部药学院,江苏苏州215123
- 折叠
摘要
目的 研究罗丹宁衍生物Lj0104在大鼠体内的主要代谢产物.方法 对雄性SD大鼠采用口服和静脉注射两种给药方式,给药剂量为5.0 mg/kg(口服)和1.0 mg/kg(静脉注射).在24 h内眼眶取血,采用质谱方法对血浆中母体化合物及代谢产物进行分析.结果 发现Lj0104有3种主要代谢产物.结论 化合物Lj0104主要代谢为水解和羟基化产物.该研究为进一步对该化合物进行结构改造提供了实验及理论依据.
Abstract
Objective To study the metabolites of rodanine derivative Lj0104 in rat plasma in particular. Method Verapamil is utilized as the internal standard (IS). Male Sprague-Dawley rats were administered with compound Lj0104 by po. 5. 0 mg/kg and iv. 1.0 mg/kg. Plasma concentration of the parent compound and the metabolites were analyzed using LC-MS/MS. Result Three major metabolites were discovered. Conclusion The major metabolites of Lj0104 are hydroxylation and hydrolysis products. This study provides guidance for further modification of Lj0104.
关键词
罗丹宁衍生物/体内代谢产物/水解/羟基化/质谱Key words
rodanine derivative/metabolite/hydrolysis/hydroxylation/mass spectrometry引用本文复制引用
基金项目
国家重大新药创制项目(2009ZX09103-129)
江苏省第4期"333工程"第3层次人才培养项目()
出版年
2012
NETL
NSTL
维普
万方数据