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PREDOMINANT CONTRIBUTION OF ORGANIC ANION TRANSPORTING POLYPEPTIDE OATP-B (OATP2B1) TO APICAL UPTAKE OF ESTRONE-3-SULFATE BY HUMAN INTESTINAL CACO-2 CELLS
Human organic anion transporting polypeptide OATP-B (OATP2B1) is a pH-sensitive transporter expressed in the apical membranes of small intestinal epithelial cells. In this study, we have examined theExpand
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The effects of the SLCO2B1 c.1457C>T polymorphism and apple juice on the pharmacokinetics of fexofenadine and midazolam in humans
Objective The objective was to determine the effects of the SLCO2B1 c.1457C>T polymorphism and apple juice on the pharmacokinetics of fexofenadine and midazolam in humans. Methods Individuals wereExpand
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Oseltamivir (Tamiflu) Efflux Transport at the Blood-Brain Barrier via P-Glycoprotein
Oseltamivir (Tamiflu, Roche, Nutley, NJ), an ester-type prodrug of the anti-influenza drug Ro 64–0802 (oseltamivir carboxylate), has been reported to be associated with neuropsychiatric side effects,Expand
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Effect of Plasma Protein Binding on in Vitro-in Vivo Correlation of Biliary Excretion of Drugs Evaluated by Sandwich-Cultured Rat Hepatocytes
In the present study, we examined in vitro biliary clearance of several compounds in sandwich-cultured rat hepatocytes (SCRH) and compared it with that observed in vivo in rats; the effect of plasmaExpand
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Oseltamivir (Tamiflu) Is a Substrate of Peptide Transporter 1
Oseltamivir, an ester-type prodrug of the neuraminidase inhibitor [3R,4R,5S]-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate phosphate (Ro 64-0802), has been developed for theExpand
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Effects of one-time apple juice ingestion on the pharmacokinetics of fexofenadine enantiomers
PurposeWe examined the effect of a single apple juice intake on the pharmacokinetics of fexofenadine enantiomers in healthy Japanese subjects.MethodsIn a randomized two phase, open-label crossoverExpand
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TRANSPORT OF THE DOPAMINE D2 AGONIST PRAMIPEXOLE BY RAT ORGANIC CATION TRANSPORTERS OCT1 AND OCT2 IN KIDNEY
We investigated the mechanism of renal tubular secretion of the dopamine D2 receptor agonist pramipexole in rats, focusing on organic cation transporters 1 and 2. The uptake of [14C]pramipexole byExpand
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EFFECT OF P-GLYCOPROTEIN ON INTESTINAL ABSORPTION AND BRAIN PENETRATION OF ANTIALLERGIC AGENT BEPOTASTINE BESILATE
The antiallergic agent bepotastine besilate is a nonsedating, second-generation H1-antagonist with high oral absorption and negligible distribution into brain. To clarify the role of P-glycoproteinExpand
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Cloning of the dog bile salt export pump (BSEP; ABCB11) and functional comparison with the human and rat proteins
The dog bile salt export pump (BSEP; ABCB11) was cloned and expressed in a Sf9 insect cell system. The deduced amino acid sequence encodes a 1325‐amino‐acid protein, which shows 89.4% and 80.2%Expand
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P‐gp activity and inhibition in the different regions of human intestine ex vivo
Although intestinal P-glycoprotein (P-gp) has been extensively studied in vitro and in animals, its activity and the consequences of P-gp inhibition for drug disposition and toxicity in humans areExpand
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