Synthesis and in vivo evaluation of [(11)C]CGP62349, a new GABA(B) receptor antagonist

Nucl Med Biol. 2000 Aug;27(6):565-9. doi: 10.1016/s0969-8051(00)00124-4.

Abstract

This paper describes the radiosynthesis of [(11)C]CGP62349, a potential ligand to assess GABA(B) receptors in vivo. (11)C was introduced by O-methylation of the corresponding des-methyl precursor, namely CGP67780. The final product was obtained with a reliable method in good yield. The radioligand was tested in monkey, revealing negligible blood-brain barrier penetration and brain uptake, thus prompting us to search for a new target structure with a better lipophilicity.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzoates / blood
  • Benzoates / chemical synthesis*
  • Benzoates / chemistry
  • Benzoates / pharmacokinetics*
  • Blood-Brain Barrier / drug effects
  • Brain / blood supply
  • Brain / diagnostic imaging
  • Brain / metabolism*
  • Carbon Radioisotopes / chemistry
  • Chromatography, High Pressure Liquid
  • Female
  • GABA-B Receptor Antagonists*
  • Hydrocarbons, Iodinated / chemistry
  • Ligands
  • Macaca nemestrina
  • Mass Spectrometry
  • Organophosphorus Compounds / blood
  • Organophosphorus Compounds / chemical synthesis*
  • Organophosphorus Compounds / pharmacokinetics*
  • Phosphinic Acids / chemistry
  • Radioactive Tracers
  • Radioligand Assay
  • Receptors, GABA-B / metabolism
  • Tomography, Emission-Computed

Substances

  • Benzoates
  • CGP 62349
  • CGP 67780
  • Carbon Radioisotopes
  • GABA-B Receptor Antagonists
  • Hydrocarbons, Iodinated
  • Ligands
  • Organophosphorus Compounds
  • Phosphinic Acids
  • Radioactive Tracers
  • Receptors, GABA-B
  • methyl iodide