Conference Presentation (After Call) FZJ-2024-04014

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A1 adenosine receptor occupancy and availability after 5-day regular coffee consumption and subsequent abstention

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2022

60. Jahrestagung der Deutschen Gesellschaft für Nuklearmedizin, LeipzigLeipzig, Germany, 27 Apr 2022 - 30 Apr 20222022-04-272022-04-30 [10.1055/s-0042-1746012]

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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.


Contributing Institute(s):
  1. Nuklearchemie (INM-5)
  2. Molekulare Organisation des Gehirns (INM-2)
Research Program(s):
  1. 5253 - Neuroimaging (POF4-525) (POF4-525)

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 Record created 2024-06-21, last modified 2024-06-26



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