Why the study?
SUR1 overexpression in the central nervous system is a potential biomarker for PET imaging of brain damage and recovery.
The successful radiolabeling and demonstrated brain penetration of [11C]VU0071063 in rats supports its potential as a PET imaging biomarker for SUR1 overexpression in brain damage.
Supports preclinical SUR1 PET evaluation in brain injury models; leaves open clinical translation pending human validation.
Sulfonylurea receptor 1 (SUR1) overexpression in the central nervous system is a potential biomarker for positron emission tomography (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.
No takes yet. Share an insight, caveat, or question.
Caillé et al. (2021) studied this question.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: