Effects of β-blockers and tricyclic antidepressants on the activity of human organic anion transporting polypeptide 1A2 (OATP1A2).

Effects of b-Blockers and Tricyclic Antidepressants on the Activity of Human Organic Anion Transporting Polypeptide 1A2 (OATP1A2) s

The organic anion transporting polypeptide 1A2 (OATP1A2), a membrane drug transporter expressed on important organs (such as the brain, kidney, and intestine) may be a key element in the disposition of drugs. Previous studies demonstrated that it could transport a broad spectrum of substrates, including endogenous molecules and clinically relevant drugs, such as several b-blockers and 3-hydroxy...

Functional Oatp1a2 Polymorphisms and Drug Transport 1 Polymorphisms in Human Organic Anion Transporting Polypeptide 1a2 (oatp1a2): Implications for Altered Drug Disposition and Cns Drug Entry

Does Ethnic Variability Exist in the Systemic Exposures of OATP1A2 Substrates–Fexofenadine in Taiwanese?

The aim of this study was to investigate differences in organic anion transporting polypeptide 1A2 activity among the Taiwanese population via an analysis of 3 pharmacokinetic studies completed in a total of 103 healthy male Taiwanese subjects. The pharmacokinetics of fexofenadine was measured as an indicator of organic anion transporting polypeptide 1A2 activity. Using the Kolmogorov-Smirnov t...

PDZK1 and NHERF1 Regulate the Function of Human Organic Anion Transporting Polypeptide 1A2 (OATP1A2) by Modulating Its Subcellular Trafficking and Stability

The human organic anion transporting polypeptide 1A2 (OATP1A2) is an important membrane protein that mediates the cellular influx of various substances including drugs. Previous studies have shown that PDZ-domain containing proteins, especially PDZK1 and NHERF1, regulate the function of related membrane transporters in other mammalian species. This study investigated the role of PDZK1 and NHERF...

Genetic polymorphisms and function of the organic anion-transporting polypeptide 1A2 and its clinical relevance in drug disposition.

The solute carrier organic anion-transporting polypeptides (OATPs) are a family of transporter proteins that have been extensively recognized as key determinants of absorption, distribution, metabolism and excretion of various drugs because of their broad substrate specificity and wide tissue distribution as well as the involvement of drug-drug interaction. Human OATP1A2 is a drug uptake transp...