Whole-body biodistribution and radiation dosimetry of the cannabinoid type 2 receptor ligand [11C]-NE40 in healthy subjects.

Purpose: The type 2 cannabinoid receptor (CB2R) is part of the human endocannabinoid system and is involved in central and peripheral inflammatory processes. In vivo imaging of the CB2R would allow study of several (neuro)inflammatory disorders. In this study we have investigated the safety and tole...

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Publicado en:Molecular Imaging & Biology Vol. 15; no. 4; pp. 384 - 391
Autores principales: Ahmad, Rawaha, Koole, Michel, Evens, Nele, Serdons, Kim, Verbruggen, Alfons, Bormans, Guy, Van Laere, Koen
Formato: research Journal Article
Publicado: Springer Nature Aug2013
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Aug2013
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      pub: Springer Nature
      place: New York, New York
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        atl: Whole-body biodistribution and radiation dosimetry of the cannabinoid type 2 receptor ligand [11C]-NE40 in healthy subjects.
      aug:
        au:
          Ahmad, Rawaha
          Koole, Michel
          Evens, Nele
          Serdons, Kim
          Verbruggen, Alfons
          Bormans, Guy
          Van Laere, Koen
        affil: Division of Nuclear Medicine, University Hospital Leuven, Herestraat 49, 3000, Leuven, Belgium, rawaha.ahmad@uzleuven.be.
      sug:
        subj:
          Health
          Quinolines Pharmacokinetics
          Receptors, Cell Surface Metabolism
          Adult
          Aged
          Diagnostic Imaging
          Dose-Response Relationship, Radiation
          Human
          Immunity
          Laboratory Chemicals
          Male
          Middle Age
          Radiometry
          Research Subjects
          Time Factors
          Young Adult
          Adult: 19-44 years
          Aged: 65+ years
          Middle Aged: 45-64 years
          Male
      ab: Purpose: The type 2 cannabinoid receptor (CB2R) is part of the human endocannabinoid system and is involved in central and peripheral inflammatory processes. In vivo imaging of the CB2R would allow study of several (neuro)inflammatory disorders. In this study we have investigated the safety and tolerability of [11C]-NE40, a CB2R positron emission tomography (PET) ligand, in healthy human male subjects and determined its biodistribution and radiation dosimetry.Procedure: Six healthy male subjects (age 20-65 years) underwent a dynamic series of nine whole-body PET/CT scans for up to 140 min, after injection of an average bolus of 286 MBq of [11C]-NE40. Organ absorbed and total effective doses were calculated through OLINDA.Results: [11C]-NE40 showed high initial uptake in the spleen and a predominant hepatobiliary excretion. In the brain, rapid uptake and swift washout were seen. Organ absorbed doses were largest for the small intestine and liver, with 15.6 and 11.5 μGy/MBq, respectively. The mean effective dose was 3.64±0.81 μSv/MBq. There were no changes with aging observed. No adverse events were encountered.Conclusions: This first-in-man study of [11C]-NE40 showed an expected biodistribution compatible with lymphoid tissue uptake and appropriate fast brain kinetics in the healthy human brain, underscoring the potential of this tracer for further application in central and peripheral inflammation imaging. The effective dose is within the typical expected range for 11C ligands.
      pubtype: Academic Journal
      doctype:
        research
        Journal Article
      ougenre: Article
    language: English
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