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@INPROCEEDINGS{Elmenhorst:1027704,
      author       = {Elmenhorst, D. and Elmenhorst, E. and Lange, D. and Baur,
                      D. and Beer, Simone and Pierling, A. and Kroll, T. and
                      Neumaier, B. and Aeschbach, D. and Bauer, Andreas and
                      Landolt, H.},
      title        = {{A}1 adenosine receptor occupancy and availability after
                      5-day regular coffee consumption and subsequent abstention},
      reportid     = {FZJ-2024-04014},
      year         = {2022},
      abstract     = {Ziel/Aim The stimulating effects of commonly consumed
                      caffeine, the majorpsychostimulant ingredient of coffee, are
                      evoked through non-selective antagonismat adenosine
                      receptors. [F-18]CPFPX is a highly selective and affine
                      ligandat the A1 adenosine receptor (A1AR) and has been
                      successfully implementedas PET ligand. Here, we quantified
                      by [F-18]CPFPX PET the in vivo brainoccupancy of A1AR after
                      short-term coffee consumption during sleep restrictionand
                      subsequent abstinence in the human brain.Methodik/Methods
                      Nine healthy volunteers (29 ± 5 years, 4f/5m) completedan
                      8-day in-lab study including 3 x 110-min bolus plus constant
                      infusion [F-18]CPFPX PET experiments. After a baseline PET
                      scan in the afternoon following 2weeks of caffeine
                      abstinence, participants consumed freshly brewed coffee for5
                      consecutive days, while time in bed was restricted to 5 h
                      per night. The administeredcoffee contained 200 mg caffeine
                      at 7:30 h and 100 mg caffeine at14:00 h. Subsequent PET
                      scans were conducted at the same time of day as inbaseline,
                      roughly 7 h after final coffee intake in the morning and
                      after ~ 31 hof coffee abstention including an 8h-sleep
                      episode. Metabolite corrected bloodsamples were used to
                      calculate steady-state distribution volumes (VT)
                      (i.e.,50-100 min after start of [F-18]CPFPX administration).
                      Caffeine levels in salivawere determined regularly.
                      Occupancy levels were calculated by applying theLassen plot
                      including cortical and subcortical areas, cerebellum and
                      pons.Ergebnisse/Results Dependent on the resulting plasma
                      concentrations ofcaffeine, [F-18]CPFPX binding was reduced
                      between 7 and 38 $\%.$ The caffeinedoseto A1AR-occupancy
                      relation was comparable to the previously estimatedrelation
                      with an IC50 of 67 μM in plasma corresponding to 460 mg
                      caffeine per70 kg subject (approximately 4.5 cups of
                      coffee). One day after coffee abstention,VT values did not
                      differ from baseline.Schlussfolgerungen/Conclusions Our
                      preliminary data suggest that the consumptionof 3 cups of
                      coffee for 5 days does not alter A1AR brain
                      availabilityafter 24h hours of caffeine abstention.},
      month         = {Apr},
      date          = {2022-04-27},
      organization  = {60. Jahrestagung der Deutschen
                       Gesellschaft für Nuklearmedizin,
                       Leipzig (Germany), 27 Apr 2022 - 30 Apr
                       2022},
      subtyp        = {After Call},
      cin          = {INM-5 / INM-2},
      cid          = {I:(DE-Juel1)INM-5-20090406 / I:(DE-Juel1)INM-2-20090406},
      pnm          = {5253 - Neuroimaging (POF4-525)},
      pid          = {G:(DE-HGF)POF4-5253},
      typ          = {PUB:(DE-HGF)6},
      doi          = {10.1055/s-0042-1746012},
      url          = {https://juser.fz-juelich.de/record/1027704},
}