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Biodistribution and Radiation Dosimetry of the Serotonin Transporter Ligand ¹¹C-DASB Determined from Human Whole-Body PET

Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland

¹¹C-Labeled 3-amino-4-(2-dimethylaminomethylphenylsulfanyl)-benzonitrile (DASB) is a selective radioligand for the in vivo quantitation of serotonin transporters (SERTs) using PET. The goal of this study was to provide dosimetry estimates for ¹¹C-DASB based on human whole-body PET. Methods: Dynamic whole-body PET scans were acquired for 7 subjects after the injection of 669 ± 97 MBq (18.1 ± 2.6 mCi) of ¹¹C-DASB. The acquisition for each subject was obtained at 14 time points for a total of 115 min after injection of the radioligand. Regions of interest were placed over compressed planar images of source organs that could be visually identified to generate time–activity curves. Radiation burden to the body was calculated from residence times of these source organs using the MIRDOSE3.1 program. Results: The organs with high radiation burden included the lungs, urinary bladder wall, kidneys, gallbladder wall, heart wall, spleen, and liver. The activity peaked within 10 min after the injection of ¹¹C-DASB for all these organs except two—the excretory organs gallbladder and urinary bladder wall, which had peak activities at 32 and 22 min, respectively. Monoexponential fitting of activity overlying the urinary bladder suggested that approximately 12% of activity was excreted via the urine. Simulations in which the urinary voiding interval was decreased from 4.8 to 0.6 h produced only modest effects on the dose to the urinary bladder wall. With a 2.4-h voiding interval, the calculated effective dose was 6.98 µGy/MBq (25.8 mrem/mCi). Conclusion: The estimated radiation burden of ¹¹C-DASB is relatively modest and would allow multiple PET examinations of the same research subject per year.

Key Words: ¹¹C-DASB • serotonin transporter • dosimetry • whole-body biodistribution • PET

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