Radiosynthesis of novel carbon-11-labeled triaryl ligands for cannabinoid-type 2 receptor

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1565-8. doi: 10.1016/j.bmcl.2010.01.074. Epub 2010 Jan 21.

Abstract

Two novel triaryl ligands 2 and 5 with potent in vitro binding affinities for the cannabinoid subtype-2 (CB2) receptor were labeled with a positron-emitting radioactive nuclide (11)C. Radioligands [(11)C]2, [(11)C]5, and their analogs [(11)C]3 and [(11)C]4 were synthesized by O-[(11)C]methylation of their corresponding phenol precursors with [(11)C]CH(3)I. [(11)C]2-5 had relatively high uptakes (>1.2% injected dose/g tissue) in mouse brains.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biphenyl Compounds / chemical synthesis*
  • Biphenyl Compounds / chemistry
  • Brain / diagnostic imaging
  • Carbon Radioisotopes
  • Ligands
  • Mice
  • Positron-Emission Tomography
  • Protein Binding
  • Radiography
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Receptor, Cannabinoid, CB2 / metabolism*
  • Thiophenes / chemical synthesis*
  • Thiophenes / chemistry

Substances

  • Biphenyl Compounds
  • Carbon Radioisotopes
  • Ligands
  • Radiopharmaceuticals
  • Receptor, Cannabinoid, CB2
  • Thiophenes