Dextromethorphan metabolite profiles generated by in-capillary microreaction and subsequent electrophoretic separation
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| Year of publication | 2010 |
| Type | Conference abstract |
| MU Faculty or unit | |
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| 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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