11 C-glyburide PET imaging unveils the negligible brain penetration of glyburide in humans

Abstract : Kimberly and coworkers reported the beneficial effects of intravenous glyburide on the clinical outcome of brain edema. We developed the carbon-11 radiolabeled analogue of glyburide to study the body distribution of this compound using PET imaging. In a healthy subject, the brain distribution of 11C-glyburide matched the cerebral blood volume suggesting negligible blood-brain barrier (BBB) penetration. This clinical observation corroborates preclinical findings suggesting that local changes in BBB structure and function are required for targeted delivery and favorable effects of glyburide to the injured brain tissue while minimizing potential side effects to the healthy brain.