Radiolabeling and brain penetration of [11C]VU0071063, a ligand of type 1 sulfonylurea receptors for positron emission tomography imaging. (30th November 2021)

• Record Type: Journal Article
• Authors: Caillé, Fabien; Saba, Wadad; Goutal, Sébastien; Breuil, Louise; Kuhnast, Bertrand; Tournier, Nicolas
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 65:Number 2(2022)
• Page Start: 28
• Page End: 35
• Publication Date: 2021-11-30
• Subjects: carbon‐11 radiolabeling -- PET imaging -- sulfonylurea receptors 1; Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3957
• Languages: English
• ISSNs: 0362-4803

Abstract

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. Abstract : Automated isotopic carbon‐11 radiolabeling of SURI ligand VU0071063 was successfully developed to demonstrate in vivo the brain penetration of this tracer in healthy rats using PET imaging.