Article
Stereoselective metabolism of racemic carvedilol by UGT1A1 and UGT2B7, and effects of mutation of these enzymes on glucuronidation activity.
Biological & pharmaceutical bulletin - 1 Nov 2007
Takekuma Yoh, Takenaka Toru, Yamazaki Koujiro, Ueno Kazuyuki, Sugawara Mitsuru
Abstract excerpt
Carvedilol, an alpha- and beta-adrenergic blocking drug, is mainly metabolized by CYP2D6, UGT1A1, UGT2B4 and UGT2B7. This drug is administered orally as a racemic mixture of R(+)- and S(-)-enantiomers. It has been reported that CYP2D6 prefers metabolizing S-carvedilol to R-carvedilol stereoselectively. On the other hand, stereoselective metabolism of carvedilol by UGTs is still unclear. Moreover, we have reported...
Topics
- Carbazoles
- Carvedilol
- Glucuronosyltransferase
- HeLa Cells
- Humans
- Isoenzymes
- Microsomes, Liver
- Molecular Structure
- Mutation
- Propanolamines
- Recombinant Proteins
- Stereoisomerism
