Characterization of in vitro metabolites from human liver microsomes using directly coupled hplc-nmr: Application to a phenoxathiin monoamine oxidase-A inhibitor

被引:21
作者
Shockcor, JP
Silver, IS
Wurm, RM
Sanderson, PN
Farrant, RD
Sweatman, BC
Lindon, JC
机构
[1] WELLCOME RES LABS,RES TRIANGLE PK,NC 27706
[2] WELLCOME RES LABS,DEPT PHYS SCI,BECKENHAM BR3 3BS,KENT,ENGLAND
关键词
D O I
10.3109/00498259609046687
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. The metabolism of 1-ethylphenoxathiin-10,10-dioxide (BW1370U87), an experimental compound designed as an inhibitor of monoamine oxidase-A for use as a possible anti-depression agent, has been studied in a human liver microsome preparation. 2. The identities of the metabolites have been determined using directly coupled hplc-H-1 nmr at 600 MHz in the stop-flow mode in this first study of in vitro xenobiotic metabolism using hplc-nmr. 3. The xenobiotic substances that were identified comprised the parent compound BW1370U87 (with -CH2CH3 at C1) together with sidechain-oxidized metabolites with C1 substituents of -CHOH.CH3, -CH2.CH2OH, -CHOH.CH2OH and -CH2.COOH, plus the unsubstituted phenoxathiin-10,10-dioxide.
引用
收藏
页码:41 / 48
页数:8
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