Human biodistribution and dosimetry of the SPECT benzodiazepine receptor radioligand iodine-123-iomazenil

H M Dey, J P Seibyl, J B Stubbs, S S Zoghbi, R M Baldwin, E O Smith, I G Zubal, Y Zea-Ponce, C Olson, D S Charney, H M Dey, J P Seibyl, J B Stubbs, S S Zoghbi, R M Baldwin, E O Smith, I G Zubal, Y Zea-Ponce, C Olson, D S Charney

Abstract

SPECT imaging of the brain with [123I]iomazenil has shown avid uptake of the radioligand in a distribution consistent with benzodiazepine receptor binding. The purposes of this study were to measure the whole-body distribution of activity following i.v. administration of [123I]iomazenil and to evaluate the resulting organ radiation burdens.

Methods: Serial total body scans were obtained in healthy volunteers after thyroid blockade and demonstrated avid brain uptake of radioligand.

Results: Abdominal imaging showed significant activity retention within the urinary and gastrointestinal tracts consistent with excretion via these routes. Absorbed dose to the urinary bladder was calculated to be 0.19 mGy/MBq, to the lower large intestine 0.079 mGy/MBq, to the upper large intestine 0.066 mGy/MBq, and to the thyroid 0.063 mGy/MBq.

Conclusion: Thyroid uptake may in part have represented binding to benzodiazepine receptors, since radioligand binding to tissue homogenates prepared from human thyroid showed the presence of benzodiazepine binding sites.

Source: PubMed

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