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Review ArticleReview

Drug Transporters in the Central Nervous System: Brain Barriers and Brain Parenchyma Considerations

Gloria Lee, Shannon Dallas, Meera Hong and Reina Bendayan
Pharmacological Reviews December 2001, 53 (4) 569-596;
Gloria Lee
Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Toronto, Toronto, Ontario, Canada
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Shannon Dallas
Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Toronto, Toronto, Ontario, Canada
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Meera Hong
Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Toronto, Toronto, Ontario, Canada
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Reina Bendayan
Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Toronto, Toronto, Ontario, Canada
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Abstract

Drug transport in the central nervous system is highly regulated not only by the blood-brain and the blood-cerebrospinal fluid barriers but also in brain parenchyma. The novel localization of drug transporters in brain parenchyma cells, such as microglia and astrocytes, suggest a reconsideration of the present conceptualization of brain barriers as it relates to drug transport. That is, the cellular membranes of parenchyma cells act as a second “barrier” to drug permeability and express transporters whose properties appear similar to those localized at the conventional brain barriers. This review will focus on the molecular characteristics, localization, and substrate specificities of several classes of well known membrane drug transporters (i.e., the organic cation, organic anion, nucleoside, P-glycoprotein, and multidrug resistance proteins) in the brain. Comparisons to similar transporters localized within the peripheral system and clinical implications of the functional expression of specific drug transport families will be discussed when appropriate. Nutrient and neurotransmitter transporters, whose characteristics have been reviewed extensively elsewhere, will not be considered in this review.

Footnotes

  • ↵1 Address for correspondence: Dr. Reina Bendayan, Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Toronto, 19 Russell Street, Toronto, ON M5S 2S2, Canada. E-mail:r.bendayan{at}utoronto.ca

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Pharmacological Reviews: 53 (4)
Pharmacological Reviews
Vol. 53, Issue 4
1 Dec 2001
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Review ArticleReview

Drug Transporters in the Central Nervous System: Brain Barriers and Brain Parenchyma Considerations

Gloria Lee, Shannon Dallas, Meera Hong and Reina Bendayan
Pharmacological Reviews December 1, 2001, 53 (4) 569-596;

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Review ArticleReview

Drug Transporters in the Central Nervous System: Brain Barriers and Brain Parenchyma Considerations

Gloria Lee, Shannon Dallas, Meera Hong and Reina Bendayan
Pharmacological Reviews December 1, 2001, 53 (4) 569-596;
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  • Article
    • Abstract
    • I. Introduction
    • II. The Blood-Brain Barrier and the Choroid Plexus
    • III. Brain Parenchyma
    • IV. Methods to Quantitate Drug Transport into/out of the Central Nervous System—In Vivo and In Vitro Methods
    • V. Drug Transport Mechanisms in the Brain
    • VI. Summary
    • Acknowledgments
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