Synthesis and biological evaluation of 68Ga labeled bis-DOTA-3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide) as a PET tracer for in vivo visualization of necrosis

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3216-20. doi: 10.1016/j.bmcl.2013.03.127. Epub 2013 Apr 9.

Abstract

The aim of the present study was to develop a (68)Ga labeled bis-DOTA derivative of benzylidene-bis-indole and compare the in vivo stability and biodistribution with that of the previously reported bis-DTPA derivate for in vivo imaging of necrosis using PET. Uptake of the tracer was evaluated in a mouse model of Fas-mediated hepatic apoptosis in correlation with histochemical stainings. The novel (68)Ga labeled tracer showed an improved in vivo stability and could therefore be used for selective non-invasive imaging of necrotic cell death using PET.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Coordination Complexes / chemical synthesis*
  • Coordination Complexes / pharmacokinetics
  • Coordination Complexes / toxicity
  • Gallium Radioisotopes / chemistry
  • Half-Life
  • Heterocyclic Compounds, 1-Ring / chemistry*
  • Mice
  • Necrosis / diagnostic imaging*
  • Pentetic Acid / chemistry
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacokinetics
  • Radiopharmaceuticals / toxicity
  • Tissue Distribution / drug effects
  • fas Receptor / metabolism

Substances

  • Coordination Complexes
  • Fas protein, mouse
  • Gallium Radioisotopes
  • Heterocyclic Compounds, 1-Ring
  • Radiopharmaceuticals
  • fas Receptor
  • 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
  • Pentetic Acid