Abstract
In the treatment of various central nervous system (CNS) diseases, drugs have to cross the brain barriers (blood–brain barrier and blood–cerebrospinal fluid barrier) and reach effective concentrations in the brain. In some cases, they also have to permeate through the cellular compartments of the brain parenchyma (i.e., astrocytes, microglia, oligodendrocytes, and neurons). Endothelial cells of brain barriers and brain parenchymal cells express various drug transporter proteins, which regulate the disposition of endogenous and exogenous compounds within the CNS. ATP-binding cassette transporters and solute lipid carriers are two major superfamilies involving mostly efflux and influx transports, respectively. Localization and functional expression of these influx (i.e., OATs, OCTs, and OATPs) and efflux transporters (i.e., P-gp, MRPs, and BCRP) at the brain barriers and within brain parenchymal cells may influence the brain concentration of drugs used in the treatment of CNS diseases.
Published Version
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