The use of hepatocytes to investigate drug uptake transporters

Methods in Molecular Biology
Kazuya Maeda, Yuichi Sugiyama

Abstract

The liver plays an important role in the clearance of endogenous and exogenous compounds, including drugs. As hepatic uptake is the first step in hepatic clearance, any change in the former process directly affects the overall intrinsic hepatic clearance. Several uptake transporters are expressed on the basolateral membranes of hepatocytes and mediate the hepatic uptake of hydrophilic charged compounds that cannot easily penetrate the plasma membrane. As the substrate specificities of these individual drug transporters are broad and overlap, compounds are often recognized by multiple uptake transporters. Thus, knowledge of the contribution that each transporter makes to the hepatic uptake of a compound is important for predicting the extent to which hepatic uptake clearance will change if the activity of a specific transporter is altered by a genetic polymorphism or a drug-drug interaction. Human cryopreserved hepatocytes are now commercially available and can be used for studying hepatic uptake clearance. In this chapter, we describe a method for using isolated hepatocytes to estimate the in vivo uptake clearance of compounds and the quantitative contribution of each uptake transporter to the overall hepatic uptake of anionic ...Continue Reading

Citations

Jan 9, 2016·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Helen Jane RenaudIvan Laszlo Csanaky
Dec 25, 2015·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Sarinj FattahPieter P Annaert
Nov 7, 2016·European Journal of Drug Metabolism and Pharmacokinetics·Wen ZhangChunhua Xia
Jan 8, 2014·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Patrik LundquistTommy B Andersson
Feb 12, 2013·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Aijie ZhangKexin Liu
Oct 12, 2014·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Sarinj FattahPieter Annaert
Jun 10, 2014·Pharmacological Reports : PR·Pengyuan SunKexin Liu
Aug 17, 2020·Pharmaceutics·Péter Tátrai, Péter Krajcsi
Oct 23, 2020·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Kazuyoshi MichibaHiroyuki Kusuhara

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

Yao xue xue bao = Acta pharmaceutica Sinica
Chun-Ying GaoDa-Fang Zhong
Advanced Drug Delivery Reviews
Klaas Nico FaberPeter L M Jansen
Pharmacology & Therapeutics
Rosalinde Masereeuw, Frans G M Russel
© 2021 Meta ULC. All rights reserved