Primary active transport of peptidic endothelin antagonists by rat hepatic canalicular membrane.

@article{Akhteruzzaman1999PrimaryAT,
  title={Primary active transport of peptidic endothelin antagonists by rat hepatic canalicular membrane.},
  author={S Akhteruzzaman and Yukio Kato and Akihiro Hisaka and Yuichi Sugiyama},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1999},
  volume={288 2},
  pages={
          575-81
        }
}
The biliary excretion mechanism of three derivatives of BQ-123, an anionic cyclopentapeptide, was examined using isolated canalicular membrane vesicles (CMVs) from Sprague-Dawley rats. The uptake by CMV of BQ-485, a linear peptide, BQ-518, a cyclic peptide, and compound A, a cyclic peptide with a cationic moiety, was stimulated by ATP. An "overshoot" phenomenon and saturation were observed for the ATP-dependent uptake of these three peptides. The Michaelis-Menten constants (Km) for the uptake… CONTINUE READING

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