Production and biological evaluation of [18F]-6-thia-14-fluoro-heptadecanoic acid

Nucl Med Rev Cent East Eur. 2006;9(2):108-13.

Abstract

Background: [(18)F]-6-thia-14-fluoro-heptadecanoic acid 3b, a free fatty acid, has been used in myocardial PET imaging. In order to establish an automated synthesis module for routine production in the country, a study was performed for optimization of the production conditions as well as making modifications.

Material and methods: [(18)F]Benzyl-14-Fluoro-6-thia-heptadecanoate 2b was prepared in no-carrier-added (n.c.a) form from Benzyl-14-tosyloxy-6-thia-heptadecanoate 1 in one step at 90 degrees C in Kryptofix2.2.2/[(18)F] with acetonitrile as the solvent followed by Silica column chromatography. The radiolabelled ester 2 was then hydrolysed to yield [(18)F]-6-thia-14-fluoro-heptadecanoic 3b. The final solution was concentrated using the C(18) SPE system and administered to normal rats for biodistribution and co-incidence imaging studies.

Results: The synthesis took 15 min with overall radiochemical yield of 15-25% (EOS) and chemical-radiochemical purity of more than 90%. Automation was performed using a two-pot synthesis. The best imaging time was shown to be 140-180 minutes post injection.

Conclusions: Using this procedure a fast, reliable, automated synthesis for the cardial PET tracer, i.e. [(18)F]FTHA, can be obtained without an HPLC purification step.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Drug Evaluation, Preclinical
  • Fatty Acids / chemistry
  • Fatty Acids / pharmacokinetics*
  • Heart / diagnostic imaging*
  • Metabolic Clearance Rate
  • Myocardium / metabolism*
  • Organ Specificity
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacokinetics
  • Rats
  • Rats, Sprague-Dawley
  • Tissue Distribution

Substances

  • Fatty Acids
  • Radiopharmaceuticals
  • 14-fluoro-6-thiaheptadecanoic acid