Online-Ressource | |
Verfasst von: | Rengelshausen, Jens [VerfasserIn] |
Lindenmaier, Heike [VerfasserIn] | |
Cihlar, Tomas [VerfasserIn] | |
Walter-Sack, Ingeborg [VerfasserIn] | |
Haefeli, Walter E. [VerfasserIn] | |
Weiß, Johanna [VerfasserIn] | |
Titel: | Inhibition of the human organic anion transporter 1 by the caffeine metabolite 1-methylxanthine |
Verf.angabe: | Jens Rengelshausen, Heike Lindenmaier, Tomas Cihlar, Ingeborg Walter-Sack, Walter Emil Haefeli, and Johanna Weiss |
E-Jahr: | 2004 |
Jahr: | 5 June 2004 |
Umfang: | 5 S. |
Fussnoten: | Gesehen am 19.05.2021 |
Titel Quelle: | Enthalten in: Biochemical and biophysical research communications |
Ort Quelle: | Orlando, Fla. : Academic Press, 1959 |
Jahr Quelle: | 2004 |
Band/Heft Quelle: | 320(2004), 1, Seite 90-94 |
ISSN Quelle: | 1090-2104 |
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 ⩾100μM of 1-methylxanthine. Five hundred micromolar 1-methylxanthine was equieffective to 100μM probenecid. In contrast, caffeine and 1,7-dimethylxanthine did not inhibit the transport of 6-carboxyfluorescein at concentrations up to 500μM. 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. |
DOI: | doi:10.1016/j.bbrc.2004.05.142 |
URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt. Volltext: https://doi.org/10.1016/j.bbrc.2004.05.142 |
Volltext: https://www.sciencedirect.com/science/article/pii/S0006291X04011532 | |
DOI: https://doi.org/10.1016/j.bbrc.2004.05.142 | |
Datenträger: | Online-Ressource |
Sprache: | eng |
Sach-SW: | 1-Methylxanthine |
1,7-Dimethylxanthine | |
Caffeine | |
CHO cells | |
hOAT1 | |
Human | |
Inhibition | |
Organic anion transporter | |
K10plus-PPN: | 1758155493 |
Verknüpfungen: | → Zeitschrift |