AI Article Synopsis
- SUR1 overexpression in the brain could serve as a useful biomarker for PET imaging to assess brain injury and healing.
- VU0071063, a specialized compound that can enter the brain, was successfully labeled with carbon-11 in a single step for PET scans.
- Testing in rats showed that the compound effectively reached the brain and was quickly cleared, which supports further studies in animal models with higher SUR1 levels.
Article Abstract
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.
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| http://dx.doi.org/10.1002/jlcr.3957 | DOI Listing |
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