Sodium fluorescein is a probe substrate for hepatic drug transport mediated by OATP1B1 and OATP1B3.

@article{Bruyn2011SodiumFI,
  title={Sodium fluorescein is a probe substrate for hepatic drug transport mediated by OATP1B1 and OATP1B3.},
  author={Tom De Bruyn and Sarinj Fattah and Bruno Stieger and Patrick R Augustijns and Pieter Annaert},
  journal={Journal of pharmaceutical sciences},
  year={2011},
  volume={100 11},
  pages={
          5018-30
        }
}
The aim of this study was to characterize the in vitro hepatic uptake kinetics of sodium fluorescein (NaFluo) and identify the transporters involved. NaFluo exhibited saturable uptake kinetics in suspended rat and human hepatocytes as reflected by K(m) values of 22.5 and 14.1 µM, and V(max) values of 98.3 and 5.8 pmol/(million cells • min), respectively. Coincubation with known inhibitors (e.g. rifampicin) of organic anion transporting polypeptide (OATP/Oatp; SLCO gene family) significantly… CONTINUE READING
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