Overview of Experimental Models of the Blood‐Brain Barrier in CNS Drug Discovery

摘要: The blood-brain barrier (BBB) is a physical and metabolic entity that isolates the brain from systemic circulation. consists of tight junctions between endothelial cells contain egress transporters catabolic enzymes. To cross BBB, drug must possess appropriate physicochemical properties to achieve sufficient time-concentration profile in interstitial fluid (ISF). In this overview, we review techniques measure BBB permeation, which evidenced by free concentration compound ISF over time. We consider number measurement techniques, including vivo microdialysis receptor occupancy following perfusion. Consideration also given nonendothelial cell systems used assess both permeation test its interactions with transporters, computer models employed for predicting passive probability transporters.