Biodistribution and radiation dosimetry of the norepinephrine transporter radioligand (S,S)-[18F]FMeNER-D2: a human whole-body PET study.
OBJECTIVE
(S,S)-[(18)F]FMeNER-D(2) is a recently developed positron-emission tomography (PET) radioligand for in vivo quantification of the norepinephrine transporter system. The aim of this study was to provide dosimetry estimates for (S,S)-[(18)F]FMeNER-D(2) based on human whole-body PET measurements.


METHODS
PET scans were performed for a total of 6.4 h after the injection of 168.9 +/- 31.5 MBq of (S,S)-[(18)F]FMeNER-D(2) in four healthy male subjects. Volumes of interest were drawn on the coronal images. Estimates of the absorbed dose of radiation were calculated using the OLINDA software.


RESULTS
Uptake was largest in lungs, followed by liver, bladder, brain and other organs. Peak values of the percent injected dose (%ID) at a time after radioligand injection were calculated for the lung (21.6%ID at 0.3 h), liver (5.1%ID at 0.3 h), bladder (12.2%ID at 6 h) and brain (2.3%ID at 0.3 h). The largest absorbed dose was found in the urinary bladder wall (0.039 mGy/MBq). The calculated effective dose was 0.017 mSv/MBq.


CONCLUSIONS
Based on the distribution and dose estimates, the estimated radiation burden of (S,S)-[(18)F]FMeNER-D(2) is lower than that of [(18)F]FDG. The radioligand would allow multiple PET examinations in the same research subject per year.
Takano
Akihiro
A
Department of Clinical Neuroscience, Psychiatry Section, Karolinska Institutet, Stockholm, Sweden.
Halldin
Christer
C
Varrone
Andrea
A
Karlsson
Per
P
Sjöholm
Nils
N
Stubbs
James B
JB
Schou
Magnus
M
Airaksinen
Anu J
AJ
Tauscher
Johannes
J
Gulyás
Balázs
B
D001822:Body Burden; D006801:Humans; D008024:Ligands; D008657:Metabolic Clearance Rate; D009025:Morpholines / Q000032:analysis* / Q000493:pharmacokinetics*; D050484:Norepinephrine Plasma Membrane Transport Proteins / Q000378:metabolism*; D009928:Organ Specificity; D049268:Positron-Emission Tomography / Q000379:methods; D011829:Radiation Dosage; D011874:Radiometry; D012062:Relative Biological Effectiveness; D014018:Tissue Distribution; D051598:Whole Body Imaging / Q000379:methods*
C506462:2-(alpha-(2-fluoromethoxyphenoxy)benzyl)morpholine; D008024:Ligands; D009025:Morpholines; D050484:Norepinephrine Plasma Membrane Transport Proteins