Transformation of amoxapine by Cunninghamella elegans

被引:28
|
作者
Moody, JD
Zhang, DL
Heinze, TM
Cerniglia, CE [1 ]
机构
[1] US FDA, Natl Ctr Toxicol Res, Div Microbiol, Jefferson, AR 72079 USA
[2] US FDA, Natl Ctr Toxicol Res, Div Chem, Jefferson, AR 72079 USA
[3] Bristol Myers Squibb, Dept Metab & Pharmacokinet, Princeton, NJ 08502 USA
关键词
D O I
10.1128/AEM.66.8.3646-3649.2000
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
We examined Cunninghamella elegans to determine its ability to transform amoxapine, a tricyclic antidepressant belonging to the dibenzoxazepine class of drugs. Approximately 57% of the exogenous amoxapine was metabolized to three metabolites that were isolated by high-performance liquid chromatography and were identified by nuclear magnetic resonance and mass spectrometry as 7-hydroxyamoxapine (48%), N-formyl-7-hydroxyamoxapine (31%), and N-formylamoxapine (21%). 7-Hydroxyamoxapine, a mammalian metabolite with biological activity, now can be produced in milligram quantities for toxicological evaluation.
引用
收藏
页码:3646 / 3649
页数:4
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