• Corpus ID: 18821026

Potent bile salt and organic anion inhibition of methotrexate uptake and accumulation in the freshly isolated rat hepatocyte.

  title={Potent bile salt and organic anion inhibition of methotrexate uptake and accumulation in the freshly isolated rat hepatocyte.},
  author={David A. Gewirtz and Joyce K. Randolph and I. David Goldman},
  journal={Cancer research},
  volume={40 6},
Abstract Influx of [3H]methotrexate into freshly isolated hepatocytes is mediated by high- and low-affinity processes, both of which are inhibited by the bile salts, cholate, taurocholate, and deoxycholate, and the organic anions, bromosulfophthalein and rose bengal. At 100 µm concentrations, these compounds inhibit 1 µm [3H]methotrexate influx by 70 to 90%. Dixon plots established a similar Ki (∼20 µm) for taurocholate inhibition of the high- and low-affinity influx routes for methotrexate… 

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