Drug Metabolism and Pharmacokinetics
Online ISSN : 1880-0920
Print ISSN : 1347-4367
ISSN-L : 1347-4367
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Transcellular Transport of Creatinine in Renal Tubular Epithelial Cell Line LLC-PK1
Yumiko URAKAMINaoko KIMURAMasahiro OKUDASatohiro MASUDAToshiya KATSURAKen-ichi INUI
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2005 年 20 巻 3 号 p. 200-205

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  Background/Aim: Creatinine is excreted into urine via tubular secretion in addition to glomerular filtration. In the present study, characteristics of the creatinine transport in renal epithelial cells were investigated.
   Methods: The transcellular transport and accumulation of [14C]creatinine and [14C]tetraethylammonium (TEA) were assessed using LLC-PK1 cell monolayers cultured on porous membrane filters.
   Results: [14C]Creatinine was transported directionally from the basolateral to apical side of LLC-PK1 cell monolayers. Basolateral uptake of [14C]creatinine was dependent on membrane potential, and was saturable with apparent Km and Vmax values of 13.2±2.8 mM and 13.1±3.1 nmol/mg protein/5 min, respectively. Concomitant administration of organic cations (1 mM) such as cimetidine, quinidine and trimethoprim inhibited both the transcellular transport and accumulation of [14C]creatinine. Furthermore, apical excretion of [14C]creatinine was not dependent on acidification of the apical medium.
   Conclusions: Creatinine was subjected to directional transport across renal epithelial cells from the basolateral to apical side. The organic cation transporter should be involved in the basolateral uptake of creatinine.
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© 2005 by The Japanese Society for the Study of Xenobiotics
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