Whole-body biodistribution, radiation absorbed dose and brain SPECT imaging with iodine-123-beta-CIT in healthy human subjects.

SPECT imaging with {sup 123}I-labeled methyl 3{beta}-(4-iodophenyl)tropane-2{beta}-carboxylate ([{sup 123}I]{beta}-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 [{sup 123}]{beta}-CIT administered to eight healthy subjects were measured with attention to the accurate determination of organ time-activity data. 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 [{sup 123}I]{beta}-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 38 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 {sup 123}I. 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). Iodine-123-{beta}-CIT is a promising SPECT agent for imaging of the dopamine transporter in humans with favorable dosimetry and highmore » brain uptake. 18 refs., 4 figs., 5 tabs.« less