Why evaluate MDR1 receptor affinity in CNS pharmacokinetic assays?
MDCKII cells based in vitro system is a recommended model to evaluate blood-brain barrier permeability during CNS action novel compounds.
Toxicological evaluation of chemicals and the implications of human P-gp and BCRP transporters
Publications have confirmed the importance of developing safe chemical agents using membrane transporter analysis as a criterion. This is reflected in the field of pesticides, one of the areas in which this analysis has been most widely applied.
Cancer drug development: what to know about ABC transporters
The presence of the superfamily members of the ATP binding cassette (ABC) transporters is well established as the main cause of multidrug resistance, since they efflux therapeutic compounds from cells and reduce the intracellular drug levels.
Hepatic drug elimination: The role of OATPs and MRP2 transporters
OATP1B1 and OATP1B3 are two influx transporters of the SLCO gene family that are primarily expressed in the sinusoidal membrane of hepatocytes.
Renal elimination of drugs: The role of kidney transporters
Understanding the role of these transporters in the clearance of new molecular entities (NME) is normally performed in-vitro at the early stages of drug development.
Assessment of Drug Permeation across the Blood-Brain-Barrier (BBB) in preclinical research
The endothelial cells that conform the BBB limit the passage of blood circulating endogenous substrates and larger molecules to the brain. This intrinsic protective role is also a major hurdle for reasearchers developing drugs for Central Nervous System (CNS) disorders.
