| 生体膜輸送の分子機構に関する生物薬剤学的研究 | |
Abstract/OtherAbstract
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By incorporating the transporter-mediated or receptor-mediated transport process in physiologically based pharmacokinetic models, we succeeded in the quantitative prediction of plasma and tissue concentrations of β-lactam antibiotics, insulin, pentazocine, quinolone antibacterial agents, and inaperizone and digoxin. The author's research on transporter-mediated pharmacokinetics focuses on the molecular and functional characteristics of drug transporters such as oligopeptide transporter, monocarboxylic acid transporter, anion antiporter, organic anion transporters, organic cation/carnitine transporters (OCTNs), and the ATP-binding cassette transporters P-glycoprotein and MRP2. We have successfully demonstrated that these transporters play important roles in the influxes and/or effluxes of drugs in intestinal and renal epithelial cells, hepatocytes, and brain capillary endothelial cells that form the blood-brain barrier. In the systemic carnitine defficiency (SCD) phenotype mouse model, juvenile visceral steatosis (jvs) mouse, a mutation in the OCTN2 gene was found. Furthermore, several types of mutation in human SCD patients were found, demonstrating that OCTN2 is a physiologically important carnitine transporter. Interestingly, OCTNs transport carnitine in a sodium-dependent manner and various cationic drugs transport it in a sodium-independent manner. OCTNs are thought to be multifunctional transporters for the uptake of carnitine into tissue cells and for the elimination of intracellular organic cationic drugs. © 2002 The Pharmaceutical Society of Japan. |
Authors
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Tsuji, Akira |
Contributors
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辻, 彰 |
Publication Detail
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Publisher : 日本薬学会 Type : Journal Article Format : - |
Date Detail
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2009-02-05, 2009-02-05, 2002-12 |
Subject
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β-lactam antibiotics, Blood-brain barrier, Carnitine, Intestinal absorption, P-glycoprotein, Transporters |
Coverage
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Relation
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Source
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Copyright Information
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Other Details
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Languages : ja |
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