Evaluation of (99m)technetium-mebrofenin and (99m)technetium-sestamibi as specific probes for hepatic transport protein function in rat and human hepatocytes.

Pharmaceutical Research
B SwiftKim L R Brouwer

Abstract

This study characterized 99mTc-Mebrofenin (MEB) and 99mTc-Sestamibi (MIBI) hepatic transport and preferential efflux routes (canalicular vs. basolateral) in rat and human sandwich-cultured hepatocytes (SCH). 99mTc-MEB and 99mTc-MIBI disposition was determined in suspended hepatocytes and in SCH in the presence and absence of inhibitors and genetic knockdown of breast cancer resistance protein (Bcrp). The general organic anion transporting polypeptide (Oatp/OATP) inhibitor rifamycin SV reduced initial 99mTc-MEB uptake in rat and human suspended hepatocytes. Initial 99mTc-MIBI uptake in suspended rat hepatocytes was not Na+-dependent or influenced by inhibitors. Multidrug resistance-associated protein (Mrp2/MRP2) inhibitors decreased 99mTc-MEB canalicular efflux in rat and human SCH. 99mTc-MEB efflux in human SCH was predominantly canalicular (45.8 +/- 8.6%) and approximately 3-fold greater than in rat SCH. 99mTc-MIBI canalicular efflux was similar in human and rat SCH; basolateral efflux was 37% greater in human than rat SCH. 99mTc-MIBI cellular accumulation, biliary excretion index and in vitro biliary clearance in rat SCH were unaffected by Bcrp knockdown. 99mTc-MEB hepatic uptake is predominantly Oatp-mediated with biliary ex...Continue Reading

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Citations

Mar 14, 2013·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Brandon SwiftKim L R Brouwer
Mar 5, 2013·Expert Opinion on Drug Metabolism & Toxicology·Tom De BruynPieter Annaert
Apr 30, 2017·Journal of Pharmaceutical Sciences·Solène MarieNicolas Tournier
Dec 31, 2014·International Journal of Molecular Sciences·Pierre Bonnaventure, Catherine M Pastor
Oct 3, 2018·Chemical Biology & Drug Design·Seyed Sajad Hosseini BalefHamid Irannejad
Jan 25, 2019·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Pierre BonnaventureCatherine M Pastor
Nov 10, 2012·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Ken Grime, Stuart W Paine
Jan 18, 2020·Expert Opinion on Drug Metabolism & Toxicology·Irene Hernández Lozano, Oliver Langer
Sep 19, 2019·Scientific Reports·Masato KobayashiKeiichi Kawai
Aug 18, 2018·Contrast Media & Molecular Imaging·Catherine M Pastor
Nov 1, 2020·The Journal of Pharmacology and Experimental Therapeutics·Sagnik ChatterjeeHong Shen
Jan 22, 2021·Biochimica Et Biophysica Acta. Molecular Basis of Disease·Bruno StiegerKaspar P Locher
Mar 7, 2021·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Solène MarieNicolas Tournier

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