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

Kristof Prinsen, Lixin Jin, Kathleen Vunckx, Marijke De Saint-Hubert, Lin Zhou, Jan Cleynhens, Johan Nuyts, Guy M. Bormans, Yicheng Ni, Alfons M. Verbruggen*

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

6 Citations (Web of Science)

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.
Original languageEnglish
Pages (from-to)502-505
JournalBioorganic & Medicinal Chemistry Letters
Volume21
Issue number1
DOIs
Publication statusPublished - Jan 2011

Keywords

  • Cell death
  • Necrosis
  • Tc-99m(CO)(3)
  • SPECT
  • Benzylidene-bis-indole

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