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ABCB1 (P-glycoprotein) and blood-brain barrier: role in neurological diseases and their treatments


Journal de Pharmacie Clinique. Volume 25, Number 4, 225-35, Décembre 2006, Article original

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Author(s) : S Vautier, C Fernandez, A Milane, L Lacomblez, C Davrinche, R Farinotti

Summary : ABCB1 (MDR1/P-glycoprotein) is an ATP-dependant transmenbrane protein widely expressed in human organs, protecting them against xenobiotics. ABCB1 is involved in drug pharmacokinetics: at the blood-brain barrier level, due to its luminal localisation, ABCB1 limits drug transport and plays an important role in central detoxification. Many interindividual variabilities have been described on ABCB1 expression and functionality. Variabilities may play a role in the pathogenesis in neurological diseases. Furthermore, ABCB1 expression and/or functionality may modify drug efficacity or increase central adverse events. This paper reviews the implication of ABCB1 in the physiopathogenesis of neurological diseases and its role in the cerebral distribution of drugs.

Keywords : ABCB1, blood-brain barrier, neurological disease, neurotoxicity, genetic polymorphism, pharmacokinetics

 

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