The dosimetry of iodine-123-labeled TISCH: a SPECT imaging agent for the D1 dopamine receptor.
TISCH is an iodinated D1 specific dopamine receptor antagonist that may be useful as a SPECT imaging agent. This report documents its pharmacological safety in animals and its radiation dosimetry in humans. The dose of radiation that 123I-TISCH delivered to seven healthy subjects was estimated with the absorbed fraction technique. Conjugate images of the body were serially acquired for up to 24 hr after the administration of a known amount of activity. The count rates in the organs that could be visualized were measured on each image. These count rates were corrected for attenuation with 123I transmission scans. The doses to the other organs that did not take up enough activity to be visualized on the images were estimated with established models. The dosimetry was calculated for each subject individually before the results were averaged. Rapid biological washout minimizes the radiation exposure to most organs. The dose to the large bowel is limiting in healthy volunteers. The proximal colon receives about 0.67 rad/mCi (180 microGy/MBq) or about 5 rads for every 7.5 mCi of TISCH injected. This low radiation burden should make it feasible to study the D1 dopamine receptor in patients who have neuropsychiatric disorders before and after treatment.
Mozley
P D
PD
Department of Radiology, University of Pennsylvania, Philadelphia.
Zhu
X
X
Kung
H F
HF
Selikson
M H
MH
Hickey
J
J
Galloway
S
S
Pfieffer
N
N
Alavi
A
A
D000328:Adult; D000818:Animals; D001552:Benzazepines / Q000493:pharmacokinetics / Q000633:toxicity; D006801:Humans; D007457:Iodine Radioisotopes / Q000493:pharmacokinetics / Q000633:toxicity; D008297:Male; D011817:Rabbits; D011829:Radiation Dosage; D011954:Receptors, Dopamine / Q000032:analysis*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon
D001552:Benzazepines; D007457:Iodine Radioisotopes; D011954:Receptors, Dopamine; C067811:7-chloro-8-hydroxy-1-(3'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine