Synthesis and radiolabeling of (64)Cu-labeled 2-nitroimidazole derivative (64)Cu-BMS2P2 for hypoxia imaging

Bioorg Med Chem Lett. 2016 Mar 1;26(5):1397-400. doi: 10.1016/j.bmcl.2016.01.077. Epub 2016 Jan 28.

Abstract

The objective of this study was to develop a positron emission tomography (PET) probe with hypoxia targeting specificity and a relatively long half-life. The synthesis, (64)Cu-labeling in vitro and in vivo study of the novel 2-nitroimidazole complex (64)Cu-BMS2P2 is presented in this study. The hypoxia targeting capacity of (64)Cu-BMS2P2 in vitro was evaluated and compared with the (64)Cu-BMS181321, and confirmed by PET imaging in vivo and immunohistochemistry for carbonic anhydrase 9 (CA9) in a tumor mouse model. These results suggest that (64)Cu-BMS2P2 is a promising candidate for PET hypoxia imaging and worthy of further investigations in dynamic hypoxia imaging.

Keywords: 2-Nitroimidazole; Carbonic anhydrase 9; Copper-64; Hypoxia imaging; Positron emission tomography.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Hypoxia*
  • Coordination Complexes / chemical synthesis
  • Coordination Complexes / chemistry
  • Coordination Complexes / pharmacokinetics*
  • Copper Radioisotopes*
  • Isotope Labeling
  • Lung Neoplasms / diagnostic imaging*
  • Lung Neoplasms / pathology*
  • Mice
  • Molecular Imaging*
  • Molecular Structure
  • Neoplasms, Experimental / diagnostic imaging
  • Neoplasms, Experimental / pathology
  • Nitroimidazoles / chemical synthesis
  • Nitroimidazoles / chemistry
  • Nitroimidazoles / pharmacokinetics*
  • Positron-Emission Tomography*
  • Radiopharmaceuticals / analysis
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry

Substances

  • 64Cu-BMS2P2
  • Coordination Complexes
  • Copper Radioisotopes
  • Nitroimidazoles
  • Radiopharmaceuticals