Time-efficient and convenient synthesis of [(18)F]altanserin for human PET imaging by a new work-up procedure

Appl Radiat Isot. 2009 Nov;67(11):2040-3. doi: 10.1016/j.apradiso.2009.07.020. Epub 2009 Aug 4.


[(18)F]Altanserin, an important PET radioligand for the in vivo imaging of the 5-HT(2A) receptor, was synthesized from its precursor nitro-altanserin in DMF or DMSO at high temperatures of 150 degrees C in an overall radiochemical yield (EOB) of 23-25% after 75min. A new solid phase work-up procedure involving the acidification of the crude reaction mixture and a C18-SepPak-solid phase separation preceded the final HPLC purification. This led to a significantly reduced synthesis time as a result of a stable and early elution from the HPLC column using improved HPLC conditions (MeOH/THF/NaOAc 0.05N pH 5: 27/18/55, flow: 5 mL/min, Symetry Prep 7 microm C18 (Waters)). The synthesis was performed semi-automatically in a modified GE TracerLab synthesis module using an in-house-developed program. The synthesized [(18)F]altanserin was used in our ongoing human and animal PET imaging studies.

MeSH terms

  • Animals
  • Brain / diagnostic imaging*
  • Brain / metabolism*
  • Fluorine Radioisotopes / chemistry
  • Fluorine Radioisotopes / pharmacokinetics*
  • Humans
  • Isotope Labeling / methods
  • Ketanserin / analogs & derivatives*
  • Ketanserin / chemistry
  • Ketanserin / pharmacokinetics
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals / chemical synthesis
  • Receptor, Serotonin, 5-HT2A / metabolism*
  • Time Factors


  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • Receptor, Serotonin, 5-HT2A
  • altanserin
  • Ketanserin