• Published 2000

CYTOCHROME P 4502 C 9 IS THE PRINCIPAL CATALYST OF RACEMIC ACENOCOUMAROL HYDROXYLATION REACTIONS IN HUMAN LIVER MICROSOMES

@inproceedings{Thijssen2000CYTOCHROMEP4,
  title={CYTOCHROME P 4502 C 9 IS THE PRINCIPAL CATALYST OF RACEMIC ACENOCOUMAROL HYDROXYLATION REACTIONS IN HUMAN LIVER MICROSOMES},
  author={Henk H. W. Thijssen and Jean-Pierre Flinois and Phillippe Beaune},
  year={2000}
}
The oral anticoagulant acenocoumarol is given as a racemic mixture. The (S)-enantiomer is rapidly cleared and is the reason why only (R)-acenocoumarol contributes to the pharmacological effect. The objective of the study was to establish the cytochrome P450 (CYP) enzymes catalyzing the hydroxylations of the acenocoumarol enantiomers. Of various cDNA-expressed human CYPs, only CYP2C9 hydroxylated (S)-acenocoumarol. Hydroxylation occurred at the 6-, 7-, and 8-position with equal Km values and a… CONTINUE READING

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References

Publications referenced by this paper.
SHOWING 1-10 OF 36 REFERENCES

Biotransformation and pharmacokinetics of acenocoumarol (Sintrom®) in man

VIEW 4 EXCERPTS
HIGHLY INFLUENTIAL

Inhibition of CYP 2 C 9 by selective seretonine reuptake inhibitors : In vitro studies with tolbutamide and ( S )warfarin using human liver microsomes

  • A Hemeryck, C DeVriendt, FM Belpaire
  • Eur J Clin Pharmacol
  • 1999
VIEW 1 EXCERPT

Inhibition of CYP2C9 by selective seretonine reuptake inhibitors: In vitro studies with tolbutamide

  • A Hemeryck, C De Vriendt, FM Belpaire
  • 1999
VIEW 2 EXCERPTS

No clinically relevant effect of lornixicam intake on acenocoumarol pharmacokinetics and pharmacodynamics

  • UP Masche, KM Rentsch, A VonFelten, PJ Meier, KE Fattinger
  • Eur J Clin Pharmacol
  • 1999
VIEW 1 EXCERPT

Cytochrome P4502C9: an enzyme of major importance in human drug metabolism.

VIEW 1 EXCERPT