Simple and rapid preparation of [11C]DASB with high quality and reliability for routine applications

Appl Radiat Isot. 2009 Sep;67(9):1654-60. doi: 10.1016/j.apradiso.2009.03.005. Epub 2009 Mar 20.

Abstract

[(11)C]DASB combines all major prerequisites for a successful SERT-ligand, providing excellent biological properties and in-vivo behaviour. Thus, we aimed to establish a fully automated procedure for the synthesis and purification of [(11)C]DASB with a high degree of reliability reducing the overall synthesis time while conserving high yields and purity. The optimized [(11)C]DASB synthesis was applied in more than 60 applications with a very low failure rate (3.2%). We obtained yields up to 8.9 GBq (average 5.3+/-1.6 GBq). Radiochemical yields based on [(11)C]CH(3)I, (corrected for decay) were 66.3+/-6.9% with a specific radioactivity (A(s)) of 86.8+/-24.3 GBq/micromol (both at the end of synthesis, EOS). Time consumption was kept to a minimum, resulting in 43 min from end of bombardment to release of the product after quality control. From our data, it is evident that the presented method can be implemented for routine preparations of [(11)C]DASB with high reliability.

MeSH terms

  • Aniline Compounds / chemical synthesis*
  • Carbon Radioisotopes
  • Humans
  • Radiopharmaceuticals / chemical synthesis*
  • Serotonin Plasma Membrane Transport Proteins / agonists
  • Sulfides / chemical synthesis*

Substances

  • 3-amino-4-(2-dimethylaminomethylphenylsulfanyl)benzonitrile
  • Aniline Compounds
  • Carbon Radioisotopes
  • Radiopharmaceuticals
  • SLC6A4 protein, human
  • Serotonin Plasma Membrane Transport Proteins
  • Sulfides