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

Abstract N , N ′-bis(diethylenetriamine pentaacetic acid)-3,3′-(benzylidene)-bis-(1 H -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.