Taurolithocholate inhibits taurocholate uptake by isolated hepatocytes at low concentrations.
The cholestatic bile acid taurolithocholate inhibits taurocholate uptake by isolated liver cells non-competitively. Inhibition is instantaneous and inversely related to the cell number in the incubate. The Ki amounts to 7 micron in the presence of 2 mg cellular protein per ml. Secretion of taurocholate by isolated liver cells is not affected by taurolithocholate up to a concentration of 50 micron. This indicates a difference between the carrier for taurocholate uptake and the carrier for taurocholate secretion. Inhibition of bile acid uptake of liver cells may be involved in the pathogenesis of lithocholate-induced cholestasis.
D000818:Animals; D002793:Cholic Acids / Q000494:pharmacology*; D003864:Depression, Chemical; D066298:In Vitro Techniques; D007700:Kinetics; D008095:Lithocholic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D008099:Liver / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D051381:Rats; D013656:Taurocholic Acid / Q000378:metabolism*
D002793:Cholic Acids; D013656:Taurocholic Acid; D008095:Lithocholic Acid