Membrane Transport Mechanisms of Mizoribine in the Rat Intestine and Human Epithelial LS180 Cells(Biopharmacy)
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概要
- 論文の詳細を見る
The aim of the present study was to characterize membrane transport mechanisms of mizoribine in the intestinal epithelial cells. We evaluated the contribution of Na^+-dependent and -independent membrane transporters to mizoribine absorption in the rat intestine using an in situ closed loop method. In addition, we evaluated the effects of structurally related compounds, extracellular Na^+ concentrations, and an inhibitor of Na^+-independent equilibrative nucleoside transporter, nitrobenzylmercaptopurine ribonucleoside (NBMPR), on the uptake of mizoribine in human intestinal epithelial LS180 cells. In the presence and also absence of Na^+ in rat intestinal loops, more than 60% of the administered dose (50μg at the concentration of 100μg/ml=386μM) of mizoribine was absorbed in 40min. In the LS180 cells, ribavirin and inosine reduced the uptake of 400μM mizoribine with the increasing concentrations (from 5 to 50mM) of the inhibitors. The cellular uptake of mizoribine in the absence of extracellular Na^+ decreased to 72.7% of the uptake in the presence of extracellular Na^+, whereas 100μM NBMPR decreased the uptake of mizoribine markedly to 34.7% of that without NBMPR. These findings suggest that Na^+-independent nucleoside transporters are largely responsible for absorption of mizoribine in the intestine.
- 公益社団法人日本薬学会の論文
- 2009-04-01
著者
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TAGUCHI Masato
Graduate School of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
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HASHIMOTO Yukiya
Graduate School of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
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Hashimoto Y
Graduate School Of Pharmaceutical Sciences Kyushu University
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Hashimoto Yuichi
Institute Of Molecular & Cellular Biosciences University Of Tokyo
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Harada Yuichi
Center For Influenza Virus Research National Institute Of Infectious Diseases
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Ishida Kazuya
Graduate School Of Medicine And Pharmaceutical Sciences Univ. Of Toyama
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Taguchi Masato
Graduate School Of Medicine And Pharmaceutical Sciences Univ. Of Toyama
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Hashimoto Yukiya
Graduate School Of Medicine And Pharmaceutical Sciences Univ. Of Toyama
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TAKAAI Mari
Graduate School of Pharmaceutical Sciences, University of Toyama
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YOTSUTANI Ayano
Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama
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Hashimoto Y
Institute Of Molecular & Cellular Biosciences The University Of Tokyo
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Yotsutani Ayano
Graduate School Of Medicine And Pharmaceutical Sciences University Of Toyama
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Hashimoto Yuichi
Institute of Molecular & Cellular Biosciences, The University of Tokyo
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Takaai Mari
Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama
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