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Potent and Specific Inhibition of mMate1-Mediated Efflux of Type I Organic Cations in the Liver and Kidney by Pyrimethamine
This report describes a potent and selective inhibitor of multidrug and toxin extrusion (MATE) protein, pyrimethamine (PYR), and examines its effect on the urinary and biliary excretion of typicalExpand
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Effects of a MATE Protein Inhibitor, Pyrimethamine, on the Renal Elimination of Metformin at Oral Microdose and at Therapeutic Dose in Healthy Subjects
A microdose study of metformin was conducted to investigate the predictability of drug–drug interactions at the therapeutic dose (ThD). Healthy subjects received a microdose (100 µg) or ThD (250 mg)Expand
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Competitive Inhibition of the Luminal Efflux by Multidrug and Toxin Extrusions, but Not Basolateral Uptake by Organic Cation Transporter 2, Is the Likely Mechanism Underlying the Pharmacokinetic
Cimetidine, an H2 receptor antagonist, has been used to investigate the tubular secretion of organic cations in human kidney. We report a systematic comprehensive analysis of the inhibition potencyExpand
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Functional characterization of PCFT/HCP1 as the molecular entity of the carrier-mediated intestinal folate transport system in the rat model.
Proton-coupled folate transporter/heme carrier protein 1 (PCFT/HCP1) has recently been identified as a transporter that mediates the translocation of folates across the cellular membrane by aExpand
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Functional Characterization of Human Proton-Coupled Folate Transporter/Heme Carrier Protein 1 Heterologously Expressed in Mammalian Cells as a Folate Transporter
The functional characteristics of human proton coupled folate transporter (hPCFT)/heme carrier protein (HCP) 1 were investigated. hPCFT/HCP1 expressed transiently in human embryonic kidney 293 cellsExpand
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Prediction of Fluoroquinolone‐Induced Elevation in Serum Creatinine Levels: A Case of Drug–Endogenous Substance Interaction Involving the Inhibition of Renal Secretion
The aim of this study was to examine the mechanism underlying the elevation in serum creatinine levels caused by a novel des‐fluoro(6)‐quinolone antibacterial agent, DX‐619, in healthy subjects.Expand
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The Inhibition of Human Multidrug and Toxin Extrusion 1 Is Involved in the Drug-Drug Interaction Caused by Cimetidine
Cimetidine is known to cause drug-drug interactions (DDIs) with organic cations in the kidney, and a previous clinical study showed that coadministration of cimetidine or probenecid with fexofenadineExpand
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Molecular Identification and Functional Characterization of Rat Multidrug and Toxin Extrusion Type Transporter 1 as an Organic Cation/H+ Antiporter in the Kidney
We have cloned and functionally characterized the rat ortholog of multidrug and toxin extrusion type transporter 1 (rMATE1). The mRNA of rMATE1 was strongly expressed in kidney and detectable in theExpand
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PRIMe: A Web Site That Assembles Tools for Metabolomics and Transcriptomics
We describe a new Web site that assembles databases and tools to support research and analysis workflows ranging from metabolomics to transcriptomics. Expand
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N‐Methylnicotinamide Is an Endogenous Probe for Evaluation of Drug–Drug Interactions Involving Multidrug and Toxin Extrusions (MATE1 and MATE2‐K)
Multidrug and toxin extrusion 1 (MATE1) and MATE2‐K are H+/organic cation exchangers mediating the efflux of cationic drugs into the urine. N‐methylnicotinamide (NMN) was found to be an endogenousExpand
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