Biodistribution and radiation dosimetry in humans of [¹¹C]FLB 457, a positron emission tomography ligand for the extrastriatal dopamine D₂ receptor.
OBJECTIVE
[(11)C]FLB 457, a radioligand with very high affinity and selectivity for dopamine D2/3 receptors, is used to measure receptor binding in extrastriatal regions showing low density of the receptors. The purpose of this study was to estimate the whole-body biodistribution of radioactivity and the radiation absorbed doses to organs after intravenous injection of [(11)C]FLB 457 in healthy human subjects.


METHODS
Whole-body images were acquired for 2 h after an injection of [(11)C]FLB 457 in six healthy humans. Radiation absorbed doses were estimated by the MIRD scheme implemented in OLINDA/EXM 1.1 software.


RESULTS
Organs with the longest residence time were the liver, lungs, and brain. The organs with the highest radiation doses were the kidneys, liver, and pancreas. The effective dose delivered by [(11)C]FLB 457 is 5.9 μSv/MBq, similar to those of other (11)C-labeled tracers.


CONCLUSIONS
This effective dose would allow multiple scans in the same individual based on prevailing maximum recommended-dose guidelines in the USA and Europe.
Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan. Electronic address: y-kimura@nirs.go.jp.
Yasuyuki
Y
Kimura
Hiroshi
H
Ito
Takahiro
T
Shiraishi
Hironobu
H
Fujiwara
Fumitoshi
F
Kodaka
Harumasa
H
Takano
Hitoshi
H
Shimada
Iwao
I
Kanno
Tetsuya
T
Suhara
D000328:Adult; D005260:Female; D006801:Humans; D008024:Ligands; D008297:Male; D017072:Neostriatum / Q000000981:diagnostic imaging* / Q000378:metabolism*; D049268:Positron-Emission Tomography / Q000379:methods*; D011759:Pyrrolidines / Q000493:pharmacokinetics*; D011874:Radiometry; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D012457:Salicylamides / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D008024:Ligands; D011759:Pyrrolidines; D017448:Receptors, Dopamine D2; D012457:Salicylamides; C065065:FLB 457
Dopamine D(2) receptors; Dosimetry; Positron emission tomography; [(11)C]FLB 457