Format:
5
ISSN:
0006-291X
Content:
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.
Note:
Gesehen am 19.05.2021
In:
Biochemical and biophysical research communications, Orlando, Fla. : Academic Press, 1959, 320(2004), 1, Seite 90-94, 0006-291X
In:
volume:320
In:
year:2004
In:
number:1
In:
pages:90-94
In:
extent:5
Language:
English
DOI:
10.1016/j.bbrc.2004.05.142
URL:
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