Synthesis And Radiolabelling Of⁶⁸Ga-NOTA-Duramycin As A New Potential Apoptosis Probe Binding To PE

Objective To synthesize⁶⁸Ga-1,4,7-Triazacyclononane-1,4,7-triaceticacid-Duramycin(⁶⁸Ga-NOTA-Duramycin) and evaluate its biodistribution andefficacy in detection of apoptosis of cardiac ischemia and reperfusion injury.Methods NOTA-Duramycin was synthesized by solid phase method andlabeled with⁶⁸Ga at room temperature.Radiochemical purity and radiolabeling yieldwere analyzed by High Performance Liquid Chromatography （HPLC）.Biodistribution of⁶⁸Ga-NOTA-Duramycin in the normal mice was performed bydissection method. Cardiac ischemia and reperfusion injury in porcine models （n=6）was induced with balloon angioplasty.37MBq （1mCi）⁶⁸Ga-NOTA-Duramycin wasinjected intravenously and PET/CT images were acquired at1h postinjection. Cardiactissues were analyzed to confirm the presence of cell death.Results⁶⁸Ga-NOTA-Duramycin can be easily prepared at room temperature andhad high radiolabeling yield（92.5±2.1%） and radiochemical purity（>90%）.Intravenously injected⁶⁸Ga-NOTA-Duramycin has favorable biodistribution profiles:focal uptake in blood、 heart、 liver、 spleen、 lung and kidney were23.50±15.38,8.53±4.52,8.26±2.24,2.12±0.28,5.02±1.46,50.62±54.24ID%/g15min postinjection, and1.83±0.31,1.05±0.31,0.97±0.28,0.68±0.27,2.15±0.90,8.12±2.74ID%/g60min postinjection.It quickly cleared from the circulation via therenal system.PET/CT images detect the ischemia and reperfusion injury in porcinemodels with histologically confirmed infarction. Conclusion⁶⁸Ga-NOTA-Duramycin can be easily labeled at room temperatureand can detect myocardial apoptosis.It may be a potential radiotracer for the detectionof apoptosis.