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P-糖蛋白是ATP结合盒转运超家族成员之一,在体内许多部位均有表达,与多药耐药性有关。作为一种外排泵,血脑屏障内的P-糖蛋白能排出内源性底物和外源性化学物质以保持脑内环境的稳定,但同时也限制了治疗性药物在脑内的浓度,从而使治疗效果减弱。P-糖蛋白抑制剂可促进药物通过血脑屏障,对提高脑内药物的浓度和中枢神经系统药物的生物利用度具有重要意义。
P-glycoprotein is a member of the ATP-binding cassette transport superfamily and is expressed in many parts of the body and is associated with multidrug resistance. As an efflux pump, the P-glycoprotein within the blood-brain barrier exudes endogenous substrates and exogenous chemicals to maintain a stable brain environment but at the same time limits the concentration of the therapeutic drug in the brain , So that the treatment effect weakened. P-glycoprotein inhibitors can promote the drug through the blood-brain barrier, to improve the concentration of drugs in the brain and the central nervous system drug bioavailability of great significance.