Gepirone and 1-(2-pyrimidinyl)-piperazine in vitro: human cytochromes mediating transformation and cytochrome inhibitory effects

@article{Moltke1998GepironeA1,
  title={Gepirone and 1-(2-pyrimidinyl)-piperazine in vitro: human cytochromes mediating transformation and cytochrome inhibitory effects},
  author={Lisa L. von Moltke and David J Greenblatt and Jeffrey M. Grassi and Brian W. Granda and Steven M. Fogelman and Jerold S. Harmatz and Steven J Kramer and Louis F Fabre and Richard I. Shader},
  journal={Psychopharmacology},
  year={1998},
  volume={140},
  pages={293-299}
}
Biotransformation of gepirone to its principal metabolite, 1-(2-pyrimidinyl)-piperazine (1-PP), was studied in human liver microsomes and in microsomes from cDNA-transfected human lymphoblastoid cells. Formation of 1-PP from gepirone in liver microsomes proceeded with a mean apparent K m ranging from 335 to 677 μM. Coincubation with 1 μM ketoconazole reduced reaction velocity to less than 5% of control values at a gepirone concentration of 250 μM. Three other metabolites, presumed to be… CONTINUE READING
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