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Whole-Body Biodistribution, Radiation Absorbed Dose and Brain SPECT Imaging with Iodine-123-ß-CIT in Healthy Human Subjects

Departments of Psychiatry and Diagnostic Radiology, Yale University School of Medicine, New Haven
West Haven VA Medical Center, West Haven, Connecticut
Research Biochemicals International, Natick, Massachusetts
Oak Ridge Institute for Science and Education, Oak Ridge, Tennessee

Correspondence: For correspondence or reprints contact: John P. Seibyl, MD, Psychiatry Service, West Haven VA Medical Center/116A2, 950 Campbell Ave., West Haven, CT 06516.

ABSTRACT

SPECT imaging with ¹²³I-labeled methyl 3ß-(4-iodophenyl) tropane-2ß-carboxylate ([¹²³I]ß-CIT) in nonhuman primates has shown brain striatal activity, which primarily reflects binding to the dopamine transporter. The biodistribution and calculated radiation-absorbed doses of [¹²³I]ß-CIT administered to eight healthy subjects were measured with attention to the accurate determination of organ time-activity data. Methods: Whole-body transmission images were obtained with a scanning line source for attenuation correction of the emission images. Following administration of 92.5 ± 22.2 MBq (2.5 ± 0.6 mCi) of [¹²³I]ß-CIT, subjects were imaged with a whole-body imager every 30 min for 3 hr, every 60 min for the next 3 hr and at 12, 24 and 48 hr postinjection. Regional body conjugate counts were converted to microcuries of activity, with a calibration factor determined in a separate experiment using a distributed source of ¹²³I. Results: The peak brain uptake represented 14% of the injected dose, with 2% of the activity approximately overlying the striatal region. Highest radiation-absorbed doses were to the lung (0.1 mGy/MBq, 0.38 rads/mCi), liver (0.087 mGy/MBq, 0.32 rads/mCi) and lower large intestine (0.053 mGy/MBq, 0.20 rads/mCi). Conclusions: Iodine-123-ß-CIT is a promising SPECT agent for imaging of the dopamine transporter in humans with favorable dosimetry and high brain uptake.

Key Words: iodine-123-ß-CIT • biodistribution • SPECT • monoamine transporter • dosimetry

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