Mechanism of intestinal absorption and renal reabsorption of an orally active ace inhibitor: uptake and transport of fosinopril in cell cultures.

@article{Shu2001MechanismOI,
  title={Mechanism of intestinal absorption and renal reabsorption of an orally active ace inhibitor: uptake and transport of fosinopril in cell cultures.},
  author={Cathaleen Shu and Hong Shen and Ulrich Hopfer and David E Smith},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2001},
  volume={29 10},
  pages={1307-15}
}
The objective of this study was to delineate the transepithelial transport mechanisms of fosinopril in cultured cell lines expressing the intestinal and renal peptide transporters. Lineweaver-Burk, Dixon, and dose-response analyses revealed that GlySar uptake was competitively inhibited by fosinopril in both Caco-2 (K(i), 35.5 microM) and SKPT cells (K(i), 29.6 microM). Intracellular accumulations of fosinopril were 3 to 4 times higher from apical versus basolateral surfaces of the membrane, as… CONTINUE READING
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