The brain microvessels are formed by a specialized endothelium and regulate the movement of solutes between blood and brain. The endothelial cells are sealed together by tight junctions and play a role as the blood-brain barrier. The brain microvessels express GLUT1 as the major form of glucose transporter, aquaporin-4 as a water channel, and p-glycoprotein as a xenobiotic transporter. Occludin and claudin-5 have been identified as the components of tight junction. Increasing evidence suggests that the activities of the transporters are regulated by adrenergic nerve activity as well as by bioactive peptides such as adrenomedullin. The regulation of the activity as well as expression of these transporters may become a strategy for prophylaxis and treatment of not only cerebral vascular diseases but also neurodegenerative disorders, developmental abnormalities and aging of the brain.