Journal
DRUG DISCOVERY TODAY
Volume 6, Issue 3, Pages 150-156Publisher
ELSEVIER SCI LTD
DOI: 10.1016/S1359-6446(00)01632-9
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Penetration through the blood-brain barrier (BBB) and blood-cerebrospinal fluid barrier (BCSF B) is necessary if a drug is to achieve the required concentration for a desired pharmacological effect. Efflux transport systems at the BBB and BCSFB provide a protective barrier function by removing drugs from the brain or cerebrospinal fluid and transferring them to the systemic circulation, respectively; several transporters at the BBB and BCSFB have been identified. Efflux transport should be taken into consideration during drug development to improve brain penetration and to avoid drug-drug interactions involving these transporters and subsequent side effects.
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