Radiolabeling and preliminary biological evaluation of a (99m)Tc(CO)(3) labeled 3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide) derivative as a potential SPECT tracer for in vivo visualization of necrosis

Bioorg Med Chem Lett. 2011 Jan 1;21(1):502-5. doi: 10.1016/j.bmcl.2010.10.102. Epub 2010 Oct 26.

Abstract

N,N'-bis(diethylenetriamine pentaacetic acid)-3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide) (bis-DTPA-BI) was radiolabeled with (99m)Tc(CO)(3). The resulting (99m)Tc(CO)(3)-bis-DTPA-BI was characterized (LC-MS) and evaluated as a potential SPECT tracer for imaging of necrosis in Wistar rats with a reperfused partial liver infarction and Wistar rats with ethanol induced muscular necrosis. To study the specificity, uptake of (99m)Tc(CO)(3)-bis-DTPA-BI was also studied in a mouse model of Fas-mediated hepatic apoptosis. The obtained results indicate that (99m)Tc(CO)(3)-bis-DTPA-BI displays selective uptake in necrotic tissue and can be used for in vivo visualization of necrosis by SPECT.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis
  • Hepatocytes / pathology
  • Indoles / chemical synthesis
  • Indoles / chemistry*
  • Isotope Labeling
  • Mice
  • Necrosis / diagnosis*
  • Organotechnetium Compounds / chemistry*
  • Pentetic Acid / analogs & derivatives*
  • Pentetic Acid / chemical synthesis
  • Pentetic Acid / chemistry
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / chemistry*
  • Rats
  • Rats, Wistar
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Indoles
  • N,N'-bis(diethylenetriamine pentaacetic acid)-3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide)
  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • Pentetic Acid