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.

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.

• Authors: Kristof Prinsen, Marlein Miranda Cona, Jan Cleynhens, Hubert Vanbilloen, Junjie Li, Natalia Dyubankova, Eveline Lescrinier, Guy Bormans, Yicheng Ni, Alfons Verbruggen
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 23 Issue 11 Pg. 3216-20 (Jun 01 2013) ISSN: 1464-3405 [Electronic] England
• PMID: 23635829 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2013. Published by Elsevier Ltd.

Chemical References

• 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

Topics

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