ATP结合盒运输机
Abcg2型
血脑屏障
运输机
细胞色素P450
药理学
生物
酶
药品
化学
人脑
药物代谢
多重耐药
抗药性
CYP3A4型
流出
P-糖蛋白
CYP2B6型
基因
有机阴离子转运蛋白1
生物化学
遗传学
中枢神经系统
神经科学
作者
Xavier Declèves,Aude Jacob,Salah Yousif,Ramzi Shawahna,Sophie Potin,Jean‐Michel Scherrmann
出处
期刊:Current Drug Metabolism
[Bentham Science]
日期:2011-10-01
卷期号:12 (8): 732-741
被引量:81
标识
DOI:10.2174/138920011798357024
摘要
The recent identification of drug-metabolizing enzymes cytochrome P450 (CYP) in the human blood-brain barrier (BBB) raises the question of whether these enzymes act in concert with ATP-binding cassette (ABC) transporters to limit the brain distributions of drugs. We recently demonstrated several CYP genes in freshly isolated human brain microvessels; the main isoforms expressed were CYP1B1 and CYP2U1. Many studies using different experimental approaches have revealed that P-glycoprotein (P-gp, ABCB1), breast cancer resistance protein (BCRP, ABCG2) and the multidrug resistance-associated protein 4 (MRP4, ABCC4) are the main ABC transporters in the human BBB. The first part of this review covers recent studies on the expression, regulation and function of CYP450 and ABC transporters in the rodent and human BBBs. The second part focuses on the possible interplay between some CYPs and certain ABC transporters at the BBB, which makes it a determining element of brain drug concentrations and thus of the effects of centrally acting drugs.
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