Efflux transport systems for drugs at the blood-brain barrier and blood-cerebrospinal fluid barrier (Part 1)

Citation
H. Kusuhara et Y. Sugiyama, Efflux transport systems for drugs at the blood-brain barrier and blood-cerebrospinal fluid barrier (Part 1), DRUG DISC T, 6(3), 2001, pp. 150-156
Citations number
56
Categorie Soggetti
Pharmacology & Toxicology
Journal title
DRUG DISCOVERY TODAY
ISSN journal
13596446 → ACNP
Volume
6
Issue
3
Year of publication
2001
Pages
150 - 156
Database
ISI
SICI code
1359-6446(200102)6:3<150:ETSFDA>2.0.ZU;2-5
Abstract
Penetration through the blood-brain barrier (BBB) and blood-cerebrospinal f luid barrier (BCSF B) is necessary if a drug is to achieve the required con centration for a desired pharmacological effect. Efflux transport systems a t the BBB and BCSFB provide a protective barrier function by removing drugs from the brain or cerebrospinal fluid and transferring them to the systemi c circulation, respectively; several transporters at the BBB and BCSFB have been identified. Efflux transport should be taken into consideration durin g drug development to improve brain penetration and to avoid drug-drug inte ractions involving these transporters and subsequent side effects.