Mechanism-based inactivation of CYP2D6 by 5-fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine.

@article{Palamanda2001MechanismbasedIO,
  title={Mechanism-based inactivation of CYP2D6 by 5-fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine.},
  author={Jairam R. Palamanda and Christopher N. Casciano and Louis Arthur Norton and Robert P. Clement and Leonard V. Favreau and Charles C. Lin and Amin A. Nomeir},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2001},
  volume={29 6},
  pages={
          863-7
        }
}
SCH 66712 [5-fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine] caused a time- and NADPH-dependent loss of CYP2D6 activity. The inactivation of human liver (HL) microsomal dextromethorphan O-demethylase activity, a prototype marker for CYP2D6, was characterized by a K(I) of 4.8 microM and a maximal rate constant of inactivation (k(inact)) of 0.14 min(-1). The inactivation of the recombinant CYP2D6 in Supersomes (r-CYP2D6) was characterized by a K(I) of 0.55 microM and a k… CONTINUE READING

Citations

Publications citing this paper.
SHOWING 1-9 OF 9 CITATIONS

References

Publications referenced by this paper.
SHOWING 1-10 OF 18 REFERENCES

Enzyme Inactivation: Chemistry and Enzymology

RB Silverman
  • 1988
VIEW 3 EXCERPTS
HIGHLY INFLUENTIAL