Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER

Bioorg Med Chem Lett. 2007 Jan 15;17(2):533-7. doi: 10.1016/j.bmcl.2006.10.018. Epub 2006 Oct 12.


A series of reboxetine analogs was synthesized and evaluated for in vitro binding as racemic mixtures. The best candidate (INER) was synthesized as the optically pure (S,S) enantiomer, labeled with iodine-123 and its in vivo binding determined by SPECT imaging in baboons. The in vivo specificity, selectivity, and kinetics of [123I]INER make it a promising agent for imaging NET in vivo by noninvasive SPECT imaging.

MeSH terms

  • Adrenergic Uptake Inhibitors / chemical synthesis
  • Adrenergic Uptake Inhibitors / pharmacology
  • Animals
  • Brain Chemistry / drug effects
  • Female
  • Indicators and Reagents
  • Morpholines / chemical synthesis*
  • Morpholines / pharmacology*
  • Norepinephrine Plasma Membrane Transport Proteins / metabolism*
  • Papio
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacology*
  • Rats
  • Reboxetine
  • Stereoisomerism
  • Tomography, Emission-Computed, Single-Photon*


  • (123I)INER
  • Adrenergic Uptake Inhibitors
  • Indicators and Reagents
  • Morpholines
  • Norepinephrine Plasma Membrane Transport Proteins
  • Radiopharmaceuticals
  • Reboxetine