Synthesis of the Main Metabolite in Human Blood of the A1 Adenosine Receptor Ligand [18F]CPFPX

In human blood, the PET radiotracer [18F]CPFPX (1) is metabolized to numerous metabolites, one (M1) being the most prominent in plasma 30 min p.i. Because the mass of injected tracer is ≤5 nmol, concentrations in plasma are too low to analyze. Human liver microsomes generate main metabolites having...

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Bibliographic Details
Published in:Organic letters 2009-10, Vol.11 (19), p.4266-4269
Main Authors: Holschbach, Marcus H, Bier, Dirk, Wutz, Walter, Willbold, Sabine, Olsson, Ray A
Format: Article
Language:English
Subjects:
Cyclization
Humans
Ligands
Molecular Structure
Receptor, Adenosine A1 - blood
Receptor, Adenosine A1 - metabolism
Stereoisomerism
Xanthines - blood
Xanthines - chemical synthesis
Xanthines - metabolism
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Summary:In human blood, the PET radiotracer [18F]CPFPX (1) is metabolized to numerous metabolites, one (M1) being the most prominent in plasma 30 min p.i. Because the mass of injected tracer is ≤5 nmol, concentrations in plasma are too low to analyze. Human liver microsomes generate main metabolites having HPLC retention times identical to those in plasma. HPLC−MS tentatively identified M1 as 2. Synthesis of 2 and identical HPLC−MS spectra of 2 and M1 confirmed that assignment.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol900169f