Abstract: The structural and functional integrity of the blood-brain barrier (BBB) is a prerequisite for the maintenance of the brain homeostasis and function. Because of the structural peculiarities of the BBB, macromolecules and hydrophilic substances can pass through it only by some BBB transporter-mediated mechanisms. At the same time, the BBB is also responsible for deportation of some endogenous or exogenous substances from the brain through the efflux transporters. The current research advances on some important transporters at the BBB closely related to central nervous system (CNS) drugs, have been summarized in this review. These transporters include ABC transporters, glucose transporters, transferring receptor, insulin receptor and so on. This review offers a overview of structures, functions, distributions, relationships with CNS disease and drugs and the factors influencing their expression of some transporters at the BBB. Clarifying these elements could make a big difference to promote the CNS drugs to reach the brain across the BBB. Moreover, it provides new insights for exploring pathogenic mechanisms of some CNS diseases and their treatment.

Key words: blood-brain barrier, transporters, drug delivery, central nervous system