Evaluation of the contribution of cytochrome P450 3A4 to human liver microsomal bupropion hydroxylation.

@article{Faucette2001EvaluationOT,
  title={Evaluation of the contribution of cytochrome P450 3A4 to human liver microsomal bupropion hydroxylation.},
  author={Stephanie R. Faucette and Roy L. Hawke and Stacy Shifflett Shord and Edward L. Lecluyse and Celeste M. Lindley},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2001},
  volume={29 8},
  pages={
          1123-9
        }
}
The purpose of this investigation was to evaluate the role of cytochrome P450 (CYP) 3A4 in human liver microsomal bupropion (BUP) hydroxylation. Across the BUP concentration range of 0.075 to 12 mM, cDNA-expressed CYP3A4 demonstrated BUP hydroxylase activity only when incubated with concentrations > or =4 mM. When assayed at 12 mM BUP, cDNA-expressed CYP3A4 catalyzed BUP hydroxylation at a 30-fold lower rate than cDNA-expressed CYP2B6 (0.2 versus 7 pmol/min/pmol of P450). Among a panel of 16… CONTINUE READING

Citations

Publications citing this paper.
SHOWING 1-10 OF 27 CITATIONS

References

Publications referenced by this paper.
SHOWING 1-10 OF 29 REFERENCES

In vitro metabolism of bupropion by human liver microsomes and cDNA expressed human cytochrome P 450 ’ s ( Abstract )

  • RM Wurm, JA Dunn, IS Silver, DK Patel
  • ISSX Proc
  • 1996
Highly Influential
11 Excerpts

Similar Papers

Loading similar papers…