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

✍ Scribed by Kristof Prinsen; Lixin Jin; Kathleen Vunckx; Marijke De Saint-Hubert; Lin Zhou; Jan Cleynhens; Johan Nuyts; Guy Bormans; Yicheng Ni; Alfons Verbruggen


Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
581 KB
Volume
21
Category
Article
ISSN
0960-894X

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✦ Synopsis


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.