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

J Nucl Med. 1994 Mar;35(3):399-404.

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.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Adult
  • Brain / diagnostic imaging*
  • Female
  • Flumazenil / analogs & derivatives*
  • Humans
  • Image Processing, Computer-Assisted
  • Iodine Radioisotopes*
  • Male
  • Radiation Dosage
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon*

Substances

  • Iodine Radioisotopes
  • Flumazenil
  • iomazenil