P-糖蛋白(P-gp)是多药耐药基因编码的一种依赖ATP、能外排异物的跨膜蛋白,P-gp底物分为两大类:促进剂和抑制剂。促进剂如吗啡,可诱导P-gp表达。本文主要介绍血-脑脊液屏障上的P-gp在中枢神经系统中对阿片类药物生物利用度所起的作用,P-gp抑制剂与阿片类药物镇痛的关系及其研究进展。 P-glycoprotein (P-gp) is a transmembrane protein encoded by multidrug resistance gene that relies on ATP and can expel foreign bodies. P-gp substrates are divided into two categories: accelerators and inhibitors. Promoters such as morphine can induce P-gp expression. This article describes the role of P-gp on blood-brain barrier bioavailability of opioids in the central nervous system and the relationship between P-gp inhibitors and opioid analgesia and its progress.