Abstract

In drug discovery and development, central nervous system (CNS) drugs should be delivered into brain. Nonetheless, drug permeability into brain may be blocked by the blood-brain barrier (BBB) due to the imperviousness of the tight junction between endothelial cells in CNS and excretion by MDR1 (P-gp) expressing in the apical (luminal) membrane of endothelial cells. However, SLC transporter-mediated transport at the BBB can solve this permeable problem. It is well-known that compounds possessing N-containing groups are transported into brain across the BBB. This transportation was suggested to be associated with amine transporters. Thus, transporter-consciously designed drugs which possess N-containing groups as transporter recognition unit can be effectively delivered into brain across the BBB. In this paper, possibility of CNS drugs based on transporter-conscious drug design is described.