Abstract
N-([11C]Methyl)benperidol ([11C]NMB) can be used for PET measurements of D2-like dopamine receptor binding in vivo. We report the absorbed radiation dosimetry of i.v.-administered [11C]NMB, a critical step prior to applying this radioligand to imaging studies in humans. Whole-body PET imaging with a CTI/Siemens ECAT 953B scanner was done in a male and a female baboon. Following i.v. injection of 370-555 kBq of [11C]NMB, sequential images taken from the head to the pelvis were collected for three hours. Volumes of interest (VOIs) were identified that entirely encompassed small organs (whole brain, striatum, eyes, and myocardium). Large organs (liver, lungs, kidneys, lower large intestine, and urinary bladder) were sampled by drawing representative regions within the organ volume. Time-activity curves for each VOI were extracted from the PET and organ residence times were calculated by analytical integration of a multi-exponential fit of the time-activity curves. Human radiation doses were estimated using OLINDA/EXM 1.0 and the standard human model. Highest retention was observed in the blood and liver, each with total residence times of 1.5 min. The highest absorbed radiation doses were to the heart (10.5 μGy/MBq) and kidney (9.10 μGy/MBq), making these the critical organs for [11C]NMB. A heart absorption of 0.5 μGy would result from an injected dose of 4847 kBq [11C]NMB. Thus, up to 3700 kBq of [11C]NMB can be safely administered to human subjects for PET studies. Total body dose and effective dose for [11C]NMB are 2.8 μGy/MBq and 3.7 μSv/MBq, respectively.
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