Biliary excretion of taurolithocholate-sulfate and temocaprilat in cholestatic rats induced by bile duct-ligation and ethinylestradiol

Down-regulation of multidrug resistance protein 2 (Mrp2), a major canalicular organic anion transporter, has been reported in various cholestatic models and in patients with cholestasis. In the present study, biliary excretion of taurolithocholate-sulfate and temocaprilat, substrates of Mrp2, was st...

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Published inHepatology research Vol. 24; no. 2; p. 136
Main Authors Takikawa, Hajime, Sano, Naoyo, Onishi, Toshiki, Toda, Atsuko, Tanaka, Hiroyuki, Hojo, Makoto, Marumo, Tatsuyuki, Hanawa, Naoko, Tachizawa, Hideki, Nishikawa, Kou
Format Journal Article
LanguageEnglish
Published Netherlands 01.10.2002
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Summary:Down-regulation of multidrug resistance protein 2 (Mrp2), a major canalicular organic anion transporter, has been reported in various cholestatic models and in patients with cholestasis. In the present study, biliary excretion of taurolithocholate-sulfate and temocaprilat, substrates of Mrp2, was studied in bile duct-ligated rats and in cholestatic rats induced by ethinylestradiol (EE). Biliary excretion of temocaprilat was more markedly decreased in bile duct-ligated rats than that of taurolithocholate-sulfate. In contrast, biliary excretion of both compounds were similarly inhibited in EE-treated rat. Such difference of the degree of inhibition may have been caused by the different degree of the inhibition of unknown canalicular transporters other than Mrp2 in bile duct-ligated rats.
ISSN:1386-6346
1872-034X
DOI:10.1016/S1386-6346(02)00028-1