Genetic polymorphism in drug oxidation: in vitro studies of human debrisoquine 4-hydroxylase and bufuralol 1'-hydroxylase activities.

@article{Boobis1985GeneticPI,
  title={Genetic polymorphism in drug oxidation: in vitro studies of human debrisoquine 4-hydroxylase and bufuralol 1'-hydroxylase activities.},
  author={Alan R Boobis and Stephen Murray and C E Hampden and Donald Davies},
  journal={Biochemical pharmacology},
  year={1985},
  volume={34 1},
  pages={65-71}
}
A sensitive, specific assay utilizing fluorescence-HPLC has been developed for determining the 1'-hydroxylation of bufuralol by human liver. The 1'-hydroxylation of the isomers of bufuralol varied threefold, both the Vmax and the Km for the (+) isomer being greater than the corresponding values for the (-) isomer. Debrisoquine was a competitive inhibitor of the 1'-hydroxylation of both isomers and of the racemate of bufuralol. Both isomers and the racemate of bufuralol were competitive… CONTINUE READING

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