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

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 Wist...

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Published in:Bioorganic & medicinal chemistry letters 2011-01, Vol.21 (1), p.502-505
Main Authors: Prinsen, Kristof, Jin, Lixin, Vunckx, Kathleen, De Saint-Hubert, Marijke, Zhou, Lin, Cleynhens, Jan, Nuyts, Johan, Bormans, Guy, Ni, Yicheng, Verbruggen, Alfons
Format: Article
Language:English
Subjects:
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
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Summary: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.
ISSN:1464-3405
DOI:10.1016/j.bmcl.2010.10.102