Radiolabeling and brain penetration of [11C]VU0071063, a ligand of type 1 sulfonylurea receptors for positron emission tomography imaging |
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| Authors: | Fabien Caillé Wadad Saba Sébastien Goutal Louise Breuil Bertrand Kuhnast Nicolas Tournier |
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| Affiliation: | Inserm, CNRS, CEA, Laboratoire d'Imagerie Biomédicale Multimodale Paris-Saclay, Université Paris-Saclay, Orsay, France |
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| 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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| Keywords: | carbon-11 radiolabeling PET imaging sulfonylurea receptors 1 |
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