Clinical Pharmacokinetics

, Volume 54, Issue 3, pp 225–242 | Cite as

Drug Transporters in the Central Nervous System

Review Article
First Online:

Abstract

Drug targets in the central nervous system (CNS) are numerous and important for drug therapy, e.g., of epilepsy or pain. Drugs and other xenobiotics as well as nutrients cannot freely cross the blood–brain barrier or freely enter cells across plasma membranes and therefore require transport systems. This overview summarizes the current knowledge on the expression of drug transporters in barriers shielding the CNS from the systemic circulation and as such controlling the pharmacokinetics of drugs in the CNS. The main drug transporter families covered are SLCO, SCL22A, ABCB, and ABCC, as genes of these families code for numerous drug transporters. While knowledge on messenger RNA expression in humans, rats, and mice is remarkable, there is clearly a gap in knowledge on the subcellular expression of transporters in specific cells in the CNS and in the barriers shielding the CNS from the systemic circulation. Recent methodologic developments including synthesis of drugs and endogenous substances for imaging will in the future allow the investigation of the function and physiologic role of transporters in the CNS including difficult-to-access systems such as the choroid plexus.

Keywords

Oseltamivir Choroid Plexus Daptomycin Brain Capillary Endothelial Cell Choroid Plexus Epithelial Cell 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
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Notes

Acknowledgments

Bruno Stieger is supported by Grant No. 310030_144195 from the Swiss National Science Foundation and by the National Center of Competence in Research TransCure (University of Berne, Switzerland). Bo Gao has no conflicts of interest to declare.

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© Springer International Publishing Switzerland 2015

Authors and Affiliations

  1. 1.Department of Clinical Pharmacology and ToxicologyUniversity HospitalZurichSwitzerland

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