Investigation on the hydroxylation metabolism of imrecoxib in vitro by using recombinant human CYPs / 药学学报
Acta Pharmaceutica Sinica
;
(12): 912-915, 2005.
Article
in Chinese
| WPRIM
| ID: wpr-253542
ABSTRACT
<p><b>AIM</b>To identify the drug-metabolizing enzymes involved in the hydroxylation of the new anti-inflammatory and anodyne imrecoxib.</p><p><b>METHODS</b>Imrecoxib was incubated with heterologous expression human cytochrome P450 (rCYPs) in vitro, and metabolites and remained parent drug were detected with liquid chromatography-multistage mass spectrometry. The contribution of 4 CYPs in the hydroxylation metabolism of imrecoxib was evaluated by total normalized rate (TNR) method.</p><p><b>RESULTS</b>Imrecoxib is metabolized by CYP2C9, CYP2D6 and CYP3A4, with the rate of 62.5%, 21.1% and 16.4%, respectively.</p><p><b>CONCLUSION</b>CYP2C9 is the major enzyme involved in imrecoxib hydroxylation metabolism.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pyrroles
/
Sulfides
/
Aryl Hydrocarbon Hydroxylases
/
Cytochrome P-450 CYP2D6
/
Spectrometry, Mass, Electrospray Ionization
/
Cytochrome P-450 Enzyme System
/
Cytochrome P-450 CYP3A
/
Cyclooxygenase 2 Inhibitors
/
Cytochrome P-450 CYP2C9
/
Hydroxylation
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2005
Type:
Article
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