Much work has been done in the last several decades to improve the understanding of the molecular composition of the blood-brain barrier (BBB). Advances in magnetic resonance imaging have resulted in development of dynamic magnetic resonance imaging techniques to quantify permeability measurements across the brain endothelium. This review describes the basic anatomical and biochemical concepts of a BBB and the various techniques for magnetic resonance measurement of BBB permeability. To date, BBB permeability data have been shown to be useful in preoperative brain tumor grading and potentially also in determining the effectiveness of selective types of therapy. Explorative studies are evaluating new strategies for safe and effective altering of the BBB permeability to improve local drug delivery into brain tumors. As new antiangiogenesis drugs become available, BBB permeability imaging may also become critical as a surrogate angiogenesis marker to monitor tumor response to these agents. Finally, BBB permeability data may also prove useful in future applications to guide therapy in other nontumoral disease processes such as acute cerebral ischemia and inflammatory processes such as multiple sclerosis.