Region-dependent modulation of intestinal permeability by drug efflux transporters: in vitro studies in mdr1a(-/-) mouse intestine.

@article{Stephens2002RegiondependentMO,
  title={Region-dependent modulation of intestinal permeability by drug efflux transporters: in vitro studies in mdr1a(-/-) mouse intestine.},
  author={Richard H. Stephens and Jola Tanianis-Hughes and Norman B Higgs and Mark Humphrey and Geoff Warhurst},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2002},
  volume={303 3},
  pages={
          1095-101
        }
}
Information on the extent to which xenobiotics interact with P-glycoprotein (PGP) during transit through the intestine is crucial in determining the influence of PGP on oral drug absorption. We have recently described a novel use of isolated ileum from PGP-deficient mdr1a(-/-) mice to resolve PGP- and non-PGP-dependent drug efflux and provide a definitive measure of intrinsic drug permeability without recourse to inhibitors. The present study uses this approach to investigate the impact of PGP… CONTINUE READING

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