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
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Evaluation Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Benzoates / blood
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Benzoates / chemical synthesis*
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Benzoates / chemistry
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Benzoates / pharmacokinetics*
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Blood-Brain Barrier / drug effects
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Brain / blood supply
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Brain / diagnostic imaging
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Brain / metabolism*
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Carbon Radioisotopes / chemistry
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Chromatography, High Pressure Liquid
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Female
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GABA-B Receptor Antagonists*
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Hydrocarbons, Iodinated / chemistry
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Ligands
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Macaca nemestrina
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Mass Spectrometry
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Organophosphorus Compounds / blood
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Organophosphorus Compounds / chemical synthesis*
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Organophosphorus Compounds / pharmacokinetics*
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Phosphinic Acids / chemistry
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Radioactive Tracers
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Radioligand Assay
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Receptors, GABA-B / metabolism
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Tomography, Emission-Computed
Substances
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Benzoates
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CGP 62349
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CGP 67780
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Carbon Radioisotopes
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GABA-B Receptor Antagonists
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Hydrocarbons, Iodinated
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Ligands
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Organophosphorus Compounds
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Phosphinic Acids
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Radioactive Tracers
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Receptors, GABA-B
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methyl iodide