Comparison study of [18F]FAl-NOTA-PRGD2, [18F]FPPRGD2, and [68Ga]Ga-NOTA-PRGD2 for PET imaging of U87MG tumors in mice.
作者： Lixin Lang , Weihua Li , Ning Guo , Ying Ma , Lei Zhu
DOI: 10.1021/BC200197H
关键词:
摘要: [(18)F]FPPRGD2, an F-18 labeled dimeric cyclic RGDyK peptide, has favorable properties for PET imaging of angiogenesis by targeting the α(v)β(3) integrin receptor. This radiotracer been approved FDA use in clinical trials. However, time-consuming multiple-step synthetic procedure required its preparation may hinder widespread usage this tracer. The recent development a method using fluoride-aluminum complex to radiolabel peptides provides strategy simplifying labeling procedure. On other hand, easy-to-prepare [(68)Ga]-labeled NOTA-RGD derivatives have also reported promising receptors. purpose study was prepare [(18)F]FPPRGD2 [corrected] , [(18)F]FAl-NOTA-PRGD2, and [(68)Ga]Ga-NOTA-PRGD2 compare their pharmacokinetics tumor small animal PET. All three compounds showed rapid high tracer uptake U87MG tumors with target-to-background ratios. liver, kidneys, muscle were similar all tracers, they predominant renal clearance. In conclusion, [(18)F]FAl-NOTA-PRGD2 comparable those [(18)F]FPPRGD2. Considering ease good qualities, [(68)Ga]NOTA-PRGD2 are alternatives expression.
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