Radiolabeling and brain penetration of [11 C]VU0071063, a ligand of type 1 sulfonylurea receptors for positron emission tomography imaging

J Labelled Comp Radiopharm. 2022 Feb;65(2):28-35. doi: 10.1002/jlcr.3957. Epub 2021 Nov 30.

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.

Keywords: PET imaging; carbon-11 radiolabeling; sulfonylurea receptors 1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / diagnostic imaging
  • Carbon Radioisotopes
  • Ligands
  • Positron-Emission Tomography* / methods
  • Radiopharmaceuticals*
  • Rats
  • Sulfonylurea Receptors
  • Xanthines

Substances

  • 7-(4-(tert-butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione
  • Carbon Radioisotopes
  • Ligands
  • Radiopharmaceuticals
  • Sulfonylurea Receptors
  • Xanthines