Radiolabeling and brain penetration of [11C]VU0071063, a ligand of type 1 sulfonylurea receptors (SUR1) for PET imaging

Sulfonylurea receptor 1 (SUR1) overexpression in the central nervous system is a potential biomarker for PET imaging of brain damage and recovery. VU0071063, a selective ligand of SUR1 able to cross the blood-brain barrier, was isotopically radiolabeled with carbon-11 from a desmethyl precursor obtained quantitatively in one step. Ready-to-inject [11C]VU0071063 was obtained in 18 ± 2% radiochemical yield and 103 ± 22 GBq/μmol molar activity. PET imaging in healthy rats demonstrated a significant brain penetration and rapid elimination of the tracer in vivo, encouraging further investigation in animal models of SUR1 overexpression.