Human biodistribution and dosimetry of iodine-123-fluoroalkyl analogs of beta-CIT

Eur J Nucl Med. 1997 Nov;24(11):1422-5. doi: 10.1007/s002590050170.

Abstract

Two new N-omega-fluoroalkyl analogs of [123I]2beta-carbomethoxy-3beta-(4-iodophenyl)tropane ([123I]beta-CIT), the fluoroethyl and fluoropropyl compounds ([123I]FE-CIT and [123I]FP-CIT, respectively), have been shown to have faster kinetics and better selectivity for the dopamine transporter than [123I]beta-CIT. We examined the organ biodistribution and radiation safety of these two compounds in six healthy volunteers who received an injection with each of the two compounds 2 weeks apart. Data were obtained on the Strichman 860 whole-body scanner. Transmission scans were obtained in all subjects prior to the injection of the radiotracer with a line source and used to derive organ-specific attenuation correction factors. Whole-body planar images were acquired every hour for the first 6 h, and at 24 h. Attenuation-corrected regional conjugate counts were converted into units of activity using a calibration factor obtained for each subject by dividing whole-body conjugate decay-corrected counts from the first acquisition by the injected activity. Radiation dose estimates were on average higher for [123I]CIT-FE than for [123I]CIT-FP, with the lower large intestine receiving the highest exposure: 0.15+/-13% mGy/MBq (mean +/-COV) and 0.12+/-14% mGy/MBq for [123I]FE-CIT and [123I]FP-CIT, respectively, followed by the upper large intestine and the spleen.

Publication types

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

MeSH terms

  • Adult
  • Carrier Proteins / metabolism
  • Cocaine / analogs & derivatives*
  • Cocaine / pharmacokinetics
  • Cocaine / urine
  • Dopamine Plasma Membrane Transport Proteins
  • Female
  • Humans
  • Iodine Radioisotopes / pharmacokinetics
  • Iodine Radioisotopes / urine
  • Male
  • Membrane Glycoproteins*
  • Membrane Transport Proteins*
  • Nerve Tissue Proteins*
  • Protein Binding
  • Radiopharmaceuticals / pharmacokinetics*
  • Radiopharmaceuticals / urine
  • Radiotherapy Planning, Computer-Assisted
  • Tissue Distribution

Substances

  • Carrier Proteins
  • Dopamine Plasma Membrane Transport Proteins
  • Iodine Radioisotopes
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • Radiopharmaceuticals
  • 2beta-carbomethoxy-3beta-(4-iodophenyl)tropane
  • Cocaine