Synthesis of a novel 99mTc nitrido radiopharmaceutical with isopropyl xanthate, showing brain uptake

Appl Radiat Isot. 2009 Jan;67(1):79-82. doi: 10.1016/j.apradiso.2008.06.043. Epub 2008 Jul 22.

Abstract

In the present study, isopropyl xanthate (IPXT) ligand was labeled with the [(99m)Tc triple bond N](2+) core successfully to obtain the (99m)TcN(IPXT)(2) complex with high radiochemical purity. No decomposition of the complex at room temperature was observed over a period of 6h. Its partition coefficient indicated that it was a good lipophilic complex. The electrophoresis results showed that the complex was neutral. Biodistribution in mice demonstrated that the complex accumulated in the brain with high uptake and good retention. The brain uptake (ID%/g) was 1.95, 1.58 and 1.86 at 5-, 30- and 60-min post-injection, respectively. As compared with other reported (99m)TcN-xanthates, the (99m)TcN(IPXT)(2) complex showed higher brain uptake and better brain retention, suggesting potential usefulness of the complex as a brain perfusion imaging agent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / diagnostic imaging*
  • Brain / metabolism
  • Diagnostic Imaging
  • Drug Stability
  • Hydrophobic and Hydrophilic Interactions
  • Mice
  • Organotechnetium Compounds / chemical synthesis*
  • Organotechnetium Compounds / pharmacokinetics
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacokinetics
  • Technetium*
  • Thiones / chemistry
  • Thiones / pharmacokinetics*
  • Tissue Distribution

Substances

  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • Thiones
  • Technetium