首页> 中文期刊> 《中国药理学与毒理学杂志》 >In vitro evaluation on pharmacokinetics using a cell line expressing human renal transporters

In vitro evaluation on pharmacokinetics using a cell line expressing human renal transporters

         

摘要

cqvip:To maintain the normal physiological ionic environment,renal transporters specialize in removing waste materials,such as toxic substances,drugs and other organic cations and anions from the blood in a process of renal secretion.The purpose of this study was focused on characterizing molecular mechanisms and pharmacokinetics in renal elimination of various compounds.In this study,the development of the proximal tubule cell (S2 cell) lines stably expressing human organicanion (hOAT1,hOAT2,hOAT3 and hOAT4) and cation (hOCT1 and hOCT2) transporters were established and specific affinity of transporter for drugs is being clarified.The drug interaction between various drugs will be evaluated by measuring time- and concentration-dependent uptake and providing an exact Km and Ki value.In this presentation,the study methodology and its application using model compounds such as [^3H] riboflavin,[^3H] diazepam and [^3H] clonidine will be shown.

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