Abstract:
:The study sought to investigate the effect of genetic variants of OCT1 (OCT1-P283L and -P341L) and OCT2 (OCT2-T199I, -T201M and -A270S), which were identified in a Korean population, on the transport of lamivudine in vitro and to compare the substrate dependent effects of OCT1 and OCT2 variants with 1-methyl-4-phenylpyridinium (MPP+), tetraethyl ammonium (TEA), metformin and lamivudine as substrates for these transporters. When the transport kinetics of lamivudine uptake in oocytes overexpressing OCT1 and OCT2 wild-type (WT) and variant proteins were measured, lamivudine uptake mediated by OCT1-WT was saturable, and uptake was decreased in oocytes expressing OCT1-P283L and -P341L variants compared with that in OCT1-WT. The Clint of lamivudine in oocytes expressing OCT1-P283L was decreased by 85.1% compared with OCT1-WT, whereas it was decreased by 48.7% in oocytes expressing OCT1-P341L. The Clint of lamivudine in oocytes expressing OCT2-T199I, -T201M and -A270S was decreased by 86.2%, 88.9% and 73.6%, respectively, compared with OCT2-WT. When comparing various substrates such as MPP+, TEA, metformin and lamivudine, the effects of the OCT1 genetic polymorphisms on their uptake were not identical. However, contrary to the case of OCT1, the uptake of MPP+, TEA, metformin and lamivudine in oocytes expressing OCT2-T199I, -T201M and -A270S variants was decreased significantly compared with that in oocytes expressing OCT2-WT. In conclusion, the effect of genetic variations of OCT1 and OCT2 on the uptake of MPP+, TEA, metformin and lamivudine was substrate-dependent.
journal_name
Biopharm Drug Disposjournal_title
Biopharmaceutics & drug dispositionauthors
Choi MK,Song ISdoi
10.1002/bdd.1783subject
Has Abstractpub_date
2012-04-01 00:00:00pages
170-8issue
3eissn
0142-2782issn
1099-081Xjournal_volume
33pub_type
杂志文章abstract:AIM:The aim of this study was to build and verify a preliminary physiologically based pharmacokinetic (PBPK) model of Chinese pregnant women. The model was used to predict maternal pharmacokinetics (PK) of 6 predominantly renally cleared drugs. METHOD:Based on SimCYP Caucasian pregnancy population dataset, the prelimi...
journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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doi:10.1002/bdd.2510150508
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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abstract::The 2-oxidation activity on the pyrimidine ring of RS-8359, a MAO-A inhibitor, is the major metabolic pathway catalysed by aldehyde oxidase. This study investigated the species differences in the 2-oxidation activity by using liver cytosolic fractions from rats, mice, guinea-pigs, rabbits, dogs, monkeys and humans. Th...
journal_title:Biopharmaceutics & drug disposition
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更新日期:2006-04-01 00:00:00
abstract::Ritalin, an immediate release form of racemic methylphenidate hydrochloride, has been available in the USA since 1955 and is used for the treatment of ADHD. The objective of this study was to evaluate the pharmacokinetics of modified-release methylphenidate (highest single dose), Ritalin LA, when administered under fa...
journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
pub_type: 杂志文章
doi:10.1002/bdd.2510140608
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journal_title:Biopharmaceutics & drug disposition
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doi:10.1002/bdd.2510100106
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journal_title:Biopharmaceutics & drug disposition
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doi:10.1002/bdd.413
更新日期:2004-10-01 00:00:00
abstract::Zopiclone is a new sedative showing a rapid onset of hypnotic effect and a relatively short duration of action. The goal of this study was to assess the kinetic parameters of zopiclone and its interaction with trimipramine when administered concomitantly. Ten normal subjects each received doses of zopiclone (7.5 mg), ...
journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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abstract::In order to determine the absolute bioavailability, both oral and intravenous administrations of a drug are often used. Recently a new method has been proposed to determine absolute bioavailability in the absence of intravenous dose. Following a single oral dose, this method requires oral and renal clearance data from...
journal_title:Biopharmaceutics & drug disposition
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abstract::In situ intestinal absorption of baclofen in the rat in the presence of beta-alanine has been investigated. Through the perfusion of 0.50 mM baclofen solutions containing variable concentrations of the aminoacid (from 5 to 100 mM), a partially competitive inhibition of baclofen absorption was characterized: absorption...
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journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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abstract::The intestinal absorptive characteristics and the efflux mechanisms of candesartan (CDS), a novel angiotensin II type 1 receptor blocker, were investigated. The Caco-2 cells were used as models of the intestinal mucosa to assess uptake and transport of CDS. The determination of CDS was performed by HPLC-Flu. In the Ca...
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journal_title:Biopharmaceutics & drug disposition
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abstract::Understanding the performance of a drug product in vivo plays a key role in the development of meaningful in vitro drug release methodology. In case of functional chewing gums, the mode and the mechanism of release and the site of application differ significantly from other conventional solid oral dosage forms and req...
journal_title:Biopharmaceutics & drug disposition
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journal_title:Biopharmaceutics & drug disposition
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abstract:AIMS:To study the dose-ranging population pharmacokinetics of controlled release verapamil in healthy subjects and patients with angina or hypertension. To characterize the pharmacodynamics of controlled-release verapamil in patients with hypertension. METHODS:Dose-ranging studies were conducted in healthy volunteers ...
journal_title:Biopharmaceutics & drug disposition
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更新日期:2002-01-01 00:00:00
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更新日期:2007-05-01 00:00:00