Synthesis and characterization of a iodine-125-labeled pyrrolo[1,2-a]thieno[3,2-e]pyrazine and evaluation as a potential 5-HT4R SPECT tracer

Eur J Med Chem. 2010 Nov;45(11):5465-7. doi: 10.1016/j.ejmech.2010.07.052. Epub 2010 Aug 14.


In the aim to find new radiotracers for the in vivo imaging of 5-HT(4) receptors by ultra-high resolution quantitative SPECT, we have developed the synthesis of a radioiodinated 5-HT(4) ligand using an iododestannylation procedure. The [(125)I]-ligand was obtained in a high radiochemical yield. Preliminary autoradiographic and ex vivo studies failed to show a specific labeling of 5-HT(4) receptors.

MeSH terms

  • Chromatography, High Pressure Liquid
  • Iodine Radioisotopes / chemistry*
  • Magnetic Resonance Spectroscopy
  • Pyrazines / chemical synthesis*
  • Pyrroles / chemical synthesis*
  • Thiophenes / chemical synthesis*
  • Tomography, Emission-Computed, Single-Photon*


  • Iodine Radioisotopes
  • Pyrazines
  • Pyrroles
  • Thiophenes