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Drug transporters at brain barriers: expression and regulation by neurological disorders.

Drug transport in the central nervous system can be highly regulated by the expression of numerous influx and efflux transport proteins not only at the blood-brain barrier and blood-cerebrospinal fluid barrier but also in brain parenchymal cellular compartments (i.e., astrocytes, microglia, neurons). In particular, members of the ATP-Binding Cassette membrane-associated transporter superfamily and Solute Carrier family are known to be involved in the traffic of several endobiotics and xenobiotics (including drugs) into and out ofthe brain. These transport proteins have also been implicated in a number of neurological disorders including HIV-encephalitis, Alzheimer's disease, Parkinson's disease and neoplasia. This chapter summarizes recent knowledge on the role of drug transporters in the brain.