Preparation and evaluation of [(61)Cu]-thiophene-2-aldehyde thiosemicarbazone for PET studies

Nucl Med Rev Cent East Eur. 2008;11(2):41-7.

Abstract

Background: [(61)Cu]Thiophene-2-aldehyde thiosemicarbazone ([(61)Cu]TATS) (4) was prepared according to an analogy of carrier copper compound with antitumor activity, for eventual use in PET.

Material and methods: [(61)Cu]TATS was prepared using copper-61 acetate and in-house made ligand (TATS) in one step. (61)Cu was produced via the (nat)Zn(p,x) (61)Cu nuclear reaction (180 mircoA, 22 MeV, 3.2 h) followed by a two-step chromatography method (222 GBq of (61)Cu(2+)). [(61)Cu]TATS preparation was optimized for reaction conditions (buffer concentration and temperature). The tracer was finally administered to normal rats for biodistribution studies.

Results: Total radiolabelling of the tracer took 30 minutes with a radiochemical purity of more than 90% (using HPLC and RTLC) and specific activity of about 250-300 Ci/mmol. The complex was stable in the presence of human serum for an hour. The biodistribution of copper cation and the tracer was checked in wild-type rats for up to 2 hours with significant spleen and lung uptake of the tracer.

Conclusions: The production of (61)Cu via the (nat)Zn(p,x) (61)Cu is an efficient and reproducible method with high specific activity leading to the production and preliminary evaluation of [(61,)Cu]TATS, a potential PET tracer, was reported.

MeSH terms

  • Animals
  • Lung / diagnostic imaging
  • Lung / metabolism*
  • Metabolic Clearance Rate
  • Organ Specificity
  • Organometallic Compounds / chemistry*
  • Organometallic Compounds / pharmacokinetics*
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacokinetics
  • Rats
  • Spleen / diagnostic imaging
  • Spleen / metabolism*
  • Tissue Distribution
  • Whole Body Imaging / methods*

Substances

  • Organometallic Compounds
  • Radiopharmaceuticals