cgp-62349 and methyl-iodide

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.

Topics: Animals; Benzoates; Blood-Brain Barrier; Brain; Carbon Radioisotopes; Chromatography, High Pressure Liquid; Female; GABA-B Receptor Antagonists; Hydrocarbons, Iodinated; Ligands; Macaca nemestrina; Mass Spectrometry; Organophosphorus Compounds; Phosphinic Acids; Radioactive Tracers; Radioligand Assay; Receptors, GABA-B; Tomography, Emission-Computed