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- W2046635171 abstract "Caffeine (1,3,7-trimethylxanthine) is daily and widely consumed in beverages and food and is mainly metabolized to 1,7-dimethylxanthine and 1-methylxanthine. Indirect clinical evidence suggests that 1-methylxanthine interacts with the organic anion transport system in the human kidney. In this study the effect of caffeine and its main metabolites on the human organic anion transporter 1 (hOAT1) was investigated using CHO cells overexpressing hOAT1. The uptake of 6-carboxyfluorescein into CHOhOAT cells was significantly inhibited by ⩾100 μM of 1-methylxanthine. Five hundred micromolar 1-methylxanthine was equieffective to 100 μM probenecid. In contrast, caffeine and 1,7-dimethylxanthine did not inhibit the transport of 6-carboxyfluorescein at concentrations up to 500 μM. In conclusion, the caffeine metabolite 1-methylxanthine inhibits the transport activity of hOAT1 in vitro. The central involvement of hOAT1 in the renal excretion of numerous drugs suggests that this inhibition may alter the pharmacokinetics of a series of clinically important drugs in humans." @default.
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- W2046635171 date "2004-07-01" @default.
- W2046635171 modified "2023-10-18" @default.
- W2046635171 title "Inhibition of the human organic anion transporter 1 by the caffeine metabolite 1-methylxanthine" @default.
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- W2046635171 doi "https://doi.org/10.1016/j.bbrc.2004.05.142" @default.
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