Inhibition of microsomal phenytoin metabolism by nafimidone and related imidazoles. Potency and structural considerations.

@article{Kapetanovic1985InhibitionOM,
  title={Inhibition of microsomal phenytoin metabolism by nafimidone and related imidazoles. Potency and structural considerations.},
  author={Izet M. Kapetanovic and Harvey J. Kupferberg},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={1985},
  volume={13 4},
  pages={430-7}
}
Nafimidone and other 1-imidazoles were shown to be potent inhibitors of phenytoin p-hydroxylation in rat hepatic microsomes, being very effective even at submicromolar concentrations. The inhibitory potency of these 1-imidazoles was similar to that of SKF 525-A and considerably greater than that observed for other imidazoles (4,5-diphenylimidazole, cimetidine, metronidazole), metyrapone, or other anticonvulsants. The effects of structural modification on the inhibitory activity were examined… CONTINUE READING

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