Fig. (1). Control of drug permeation across the BBB.
Panel A) Under normal conditions, the intact BBB limits the movement of molecules into the brain. Panel B) Under pathologic conditions, the BBB becomes impaired, allowing molecules that would normally be prevented from crossing the BBB to enter the brain. Panel C) Under pathologic conditions, the endogenous channels that allow for the passage of neurotherapeutics are downregulated (i.e. Oatp1a4), limiting the efficacy of these therapies. Panel D) Pharmaceuticals aimed at upregulating these endogenous channels (i.e. Oatp1a4) are currently being investigated to improve BBB permeability to allow access of these therapeutic molecules into the brain.