Transformation of Amoxapine by Cunninghamella elegans

Author:

Moody Joanna D.1,Zhang Donglu2,Heinze Thomas M.3,Cerniglia Carl E.1

Affiliation:

1. Division of Microbiology1 and

2. Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb, Princeton, New Jersey 085022

3. Division of Chemistry,3 National Center for Toxicological Research, U.S. Food and Drug Administration, Jefferson, Arkansas 72079, and

Abstract

ABSTRACT 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.

Publisher

American Society for Microbiology

Subject

Ecology,Applied Microbiology and Biotechnology,Food Science,Biotechnology

Reference24 articles.

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