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Wolfson Brain Imaging Centre

Department of Clinical Neurosciences

Synthesis and Initial in Vivo Studies with [11C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3

WBIC PET Chemistry team has a recent publication in collaboration with Dr Peter Scott’s group in The University of Michigan Medical School.

We have developed a novel one-pot two-step method for the radiosynthesis of [11C]SB-216763 and demonstrated that it is the first radiotracer for GSK-3 able to cross the Blood-brain Barrier and enter the central nervous system in both rodents and nonhuman primates. The arylindolemaleimide skeleton represents our lead scaffold for developing a radiotracer for quantification of GSK-3 in vivo using brain PET and ultimately translating it into clinical use.


The article is published in recent journal of ACS Medicinal Chemistry Letters