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
Dans Chinois
| 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>
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Pyrroles
/
Sulfures
/
Aryl hydrocarbon hydroxylases
/
Cytochrome P-450 CYP2D6
/
Spectrométrie de masse ESI
/
Cytochrome P-450 enzyme system
/
Cytochrome P-450 CYP3A
/
Inhibiteurs de la cyclooxygénase 2
/
Cytochrome P-450 CYP2C9
/
Hydroxylation
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2005
Type:
Article
Documents relatifs à ce sujet
MEDLINE
...
LILACS
LIS