Synthesis, radiolabeling and baboon SPECT imaging of 2beta-carbomethoxy-3beta-(3'-[(123)I]iodophenyl)tropane ([(123)I]YP256) as a serotonin transporter radiotracer

Nucl Med Biol. 2008 Jan;35(1):53-9. doi: 10.1016/j.nucmedbio.2007.09.002.

Abstract

To develop a potential SPECT probe to evaluate the integrity of the serotoninergic system (5-HTT) whose dysfunction is linked to several disease conditions such as Parkinson's disease, Alzheimer's disease and depression, we report the synthesis, radiolabeling and in vivo baboon imaging of 2beta-carbomethoxy-3beta-(3'-[(123)I]iodophenyl) tropane (YP256, 6). The radiolabeling was performed by iododestannylation using sodium [(123)I]iodide and peracetic acid. Although the ligand displayed high selectivity for 5-HTT over dopamine transporter in vitro, SPECT imaging in baboons did not reveal selective 5-HTT accumulation in brain in vivo.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Brain / metabolism
  • Chromatography, High Pressure Liquid
  • Cocaine / analogs & derivatives*
  • Cocaine / chemical synthesis
  • Cocaine / metabolism
  • Female
  • Iodine Radioisotopes*
  • Isotope Labeling*
  • Papio
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / metabolism
  • Serotonin Plasma Membrane Transport Proteins / metabolism*
  • Tomography, Emission-Computed, Single-Photon*

Substances

  • 2-carbomethoxy-3-(3'-iodophenyl)tropane
  • Iodine Radioisotopes
  • Radiopharmaceuticals
  • Serotonin Plasma Membrane Transport Proteins
  • Cocaine