Substrate‐Dependent Inhibition of Human Renal Organic Cation Transporter 2 (OCT2) by Cimetidine
نویسندگان
چکیده
منابع مشابه
Kidney-specific expression of human organic cation transporter 2 (OCT2/SLC22A2) is regulated by DNA methylation.
Human organic cation transporter 2 (OCT2/SLC22A2), which is specifically expressed in the kidney, plays critical roles in the renal secretion of cationic compounds. Tissue expression and membrane localization of OCT2 are closely related to the tissue distribution, pharmacological effects, and/or adverse effects of its substrate drugs. However, the molecular mechanisms underlying the kidney-spec...
متن کاملSubstrate-dependent ligand inhibition of the human organic cation transporter OCT2.
Organic cation transporter 2 (OCT2) mediates the initial step in renal secretion of organic cations: uptake from the blood, across the basolateral membrane, and into the renal proximal tubule cells. Because of its potential as a target for unwanted drug-drug interactions (DDIs), considerable attention has been directed toward understanding the basis of OCT2 selectivity. These studies typically ...
متن کاملMetformin is a superior substrate for renal organic cation transporter OCT2 rather than hepatic OCT1.
Although metformin, a cationic agent for type II diabetes, shows its pharmacological effect in the liver, the drug is mainly eliminated into urine. The tissue selectivity based on the function of drug transporters is unclear. In the present study, the transport of metformin was examined using HEK293 cells transiently transfected with five human renal organic ion transporter cDNAs. Human OCT1 an...
متن کاملSubstrate-Dependent Inhibition of the Human Organic Cation Transporter OCT2: A Comparison of Metformin with Experimental Substrates
The importance of the organic cation transporter OCT2 in the renal excretion of cationic drugs raises the possibility of drug-drug interactions (DDIs) in which an inhibitor (perpetrator) drug decreases OCT2-dependent renal clearance of a victim (substrate) drug. In fact, there are clinically significant interactions for drugs that are known substrates of OCT2 such as metformin. To identify drug...
متن کاملPharmGKB update: I. Genetic variants of the organic cation transporter 2 (OCT2, SLC22A2).
Publications: Leabman MK, Huang CC, DeYoung J, Carlson EJ, Taylor TR, DeLaCruz M, Johns SJ, Stryke D, Kawamoto M, Urban TJ, Kroetz DL, Ferrin TE, Clark AG, Risch N, Herskowitz I, and Giacomini KM (2003) Natural variation in human membrane trasporter genes reveals evolutionary and functional constraints. Proc Natl Acad Sci (USA) 100:5896-5901. Leabman MD, Huang CC, Kawamoto M, Johns SJ, Stryke D...
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ژورنال
عنوان ژورنال: The FASEB Journal
سال: 2015
ISSN: 0892-6638,1530-6860
DOI: 10.1096/fasebj.29.1_supplement.939.10