Scherrmann Jean-Michel
INSERM U705, CNRS UMR7157, University Paris 7, University Paris 5, Hôpital Fernand Widal, 200 rue du Faubourg Saint-Denis, 75475 Paris cedex 10, France.
Expert Opin Drug Metab Toxicol. 2005 Aug;1(2):233-46. doi: 10.1517/17425255.1.2.233.
The presence of active carrier-mediated transport of substrates from the brain to the blood is a major feature of the barrier properties of the blood-brain barrier (BBB). These proteins lie in the luminal or abluminal membranes of the endothelial cells that form the BBB. Some are ATP-binding cassette proteins (ABC) and many amphipathic cationic drugs are carried by P-glycoprotein (ABCB1) or ABCG2, which lie at the luminal pole of the BBB. Several multidrug resistance-associated proteins (MRPs, ABCCs) are also present on the membranes of brain microvessels; these are mainly involved in the efflux of anionic compounds. All these ABC proteins help to protect the brain and form a critical target for CNS pharmaceuticals, influencing the clinical variability of responses to, and the design of, these drugs.
存在从大脑到血液的底物主动载体介导转运是血脑屏障（BBB）屏障特性的一个主要特征。这些蛋白质位于构成血脑屏障的内皮细胞的管腔膜或管腔外膜中。一些是ATP结合盒蛋白（ABC），许多两亲性阳离子药物由位于血脑屏障管腔极的P-糖蛋白（ABCB1）或ABCG2转运。几种多药耐药相关蛋白（MRPs，ABCCs）也存在于脑微血管膜上；这些主要参与阴离子化合物的外排。所有这些ABC蛋白有助于保护大脑，并成为中枢神经系统药物的关键靶点，影响这些药物反应的临床变异性和药物设计。
