Oxidation of dihydropyridine calcium channel blockers and analogues by human liver cytochrome P-450 IIIA4.

@article{Guengerich1991OxidationOD,
  title={Oxidation of dihydropyridine calcium channel blockers and analogues by human liver cytochrome P-450 IIIA4.},
  author={F Peter Guengerich and W. R. Brian and Masahiko Iwasaki and Matsumoto Atsuo Sari and C. B{\"a}{\"a}rnhielm and Pia S H Berntsson},
  journal={Journal of medicinal chemistry},
  year={1991},
  volume={34 6},
  pages={
          1838-44
        }
}
A series of 21 different 4-substituted 2,6-dimethyl-3-(alkoxycarbonyl)-1,4-dihydropyridines was considered with regard to oxidation to pyridine derivatives by human liver microsomal cytochrome P-450 (P-450). Antibodies raised against P-450 IIIA4 inhibited the microsomal oxidation of nifedipine and felodipine to the same extent, as did cimetidine and the mechanism-based inactivator gestodene. Gestodene was approximately 10(3) times more effective an inhibitor than cimetidine, on a molar basis… CONTINUE READING
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