RRC ID 39047
著者 Fukao M, Kondo E, Nishino H, Hattori R, Horie A, Hashimoto Y.
タイトル Presence of an H+/Quinidine Antiport System in Madin-Darby Canine Kidney Cells.
ジャーナル Eur J Drug Metab Pharmacokinet
Abstract BACKGROUND AND OBJECTIVES:We have recently found an H+/quinidine antiport system in human kidney HEK 293 cells. The aim of the present study was to evaluate whether the H+/quinidine antiport system is expressed in Madin-Darby canine kidney (MDCK) cells.
METHODS:We investigated the uptake and efflux of quinidine in MDCK cells.
RESULTS:The uptake of 100 µM quinidine into MDCK cells was decreased by acidification of extracellular pH or alkalization of intracellular pH. In addition, the uptake of quinidine was highly temperature sensitive, but was extracellular Na+ and membrane potential independent. Furthermore, tetraethylammonium, a typical substrate of renal organic cation transporters, did not inhibit the uptake of quinidine in MDCK cells. On the other hand, lipophilic cationic drugs, such as clonidine, bisoprolol, diphenhydramine, pyrilamine, and imipramine, significantly decreased the uptake of quinidine in MDCK cells. The uptake of quinidine was saturable, and the Michaelis-Menten constant was estimated to be approximately 0.5 mM. In addition, the efflux of quinidine from MDCK cells was increased by the acidification of extracellular pH, suggesting that the transport system mediates not only the uptake, but also secretion of quinidine.
CONCLUSIONS:The present findings suggested that the renal new antiport system is involved in the bidirectional membrane transport of quinidine in MDCK cells.
巻・号 41(6)
ページ 819-824
公開日 2016-12-1
DOI 10.1007/s13318-015-0314-1
PII 10.1007/s13318-015-0314-1
PMID 26628429
MeSH Absorption, Physiological / drug effects Animals Anti-Arrhythmia Agents / metabolism* Antiporters / antagonists & inhibitors Antiporters / metabolism* Biological Transport / drug effects Clonidine / pharmacology Dogs Epithelium / drug effects Epithelium / metabolism* Hot Temperature / adverse effects Hydrogen-Ion Concentration Kidney / drug effects Kidney / metabolism* Kinetics Madin Darby Canine Kidney Cells Membrane Transport Modulators / pharmacology Quinidine / metabolism* Tritium
IF 1.913
引用数 2
WOS 分野 PHARMACOLOGY & PHARMACY
リソース情報
ヒト・動物細胞 MDCK(RCB0995)