Synthesis of the main metabolite in human blood of the A1 adenosine receptor ligand [18F]CPFPX.
In human blood, the PET radiotracer [(18)F]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 < or = 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.
Holschbach
Marcus H
MH
Institute of Neuroscience and Medicine (INM-5), Forschungszentrum Jülich GmbH, D-52425 Jülich, Germany. m.holschbach@fz-juelich.de
Bier
Dirk
D
Wutz
Walter
W
Willbold
Sabine
S
Olsson
Ray A
RA
D003500:Cyclization; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D043682:Receptor, Adenosine A1 / Q000097:blood / Q000378:metabolism*; D013237:Stereoisomerism; D014970:Xanthines / Q000097:blood / Q000138:chemical synthesis* / Q000378:metabolism
C468796:8-cyclopenta-3-(3-fluoropropyl)-1-propylxanthine; D008024:Ligands; D043682:Receptor, Adenosine A1; D014970:Xanthines