Dextromethorphan metabolite profiles generated by in-capillary microreaction and subsequent electrophoretic separation

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Authors

ZEISBERGEROVÁ Marta MÁDR Aleš GLATZ Zdeněk

Year of publication 2010
Type Conference abstract
MU Faculty or unit

Faculty of Science

Citation
Description The determination of metabolite profile of potential pharmaceuticals has a substantial role in the drug development phase. For these studies human liver microsomes represent the generally accepted in vitro system. They credibly mimic liver functions as they contain many drug-metabolizing enzymes, mainly cytochromes P450 (CYPs). Alternatively, recombinant cytochrome P450 enzymes (rCYP) are suitable for frontline predictive human metabolism studies. rCYP are a favorite in vitro system for their availability and ease employment in high throughput assays. They are a valuable tool in the CYP phenotyping, i.e. searching for which CYP enzyme is involved in the biotransformation of new agents. The metabolism pathway of dextromethorphan (DEX) was chosen as a model system. DEX is an antitusive component of many medications which is chemically a non-narcotic synthetic analog of codeine. Nowadays, most of drug metabolism studies are performed by liquid chromatography-mass spectrometry methods characterized by off-line setup. However, capillary electrophoresis (CE) represents an innovative approach to perform automated enzyme assays. Different methods and procedures of enzymatic activity studies have been reported.
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