Journal of Southern Medical University ›› 2014, Vol. 34 ›› Issue (01): 51-.
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Abstract: Objective To investigate the tumor targeting efficacy of 18F-AlF-NOTA-PRGD2, a novel radiotracer ofArginine-glycine-aspartic acid (RGD) peptides. Methods 18F-AlF-NOTA-PRGD2 was synthesized in one-step by conjugatingNOTA-RGD2 with 18F-AlF at 100 ℃. The tumor targeting efficacy and in vivo biodistribution profile of 18F-AlF-NOTA-RGD2,following intravenous injection via the tail vein, were evaluated in a nude mouse model bearing subcutaneous U87MGglioblastoma xenograft by radioactivity biodistribution assessment, PET/CT and microPET/CT. Results NOTA-RGD2 was18F-fluorinated successfully in one-step with a yield of 17%-25% within 15-20 min. Radioactivity biodistribution studyconfirmed the tumor-targeting ability of 18F-AlF-NOTA-PRGD2 in the tumor-bearing mice. At 1 and 2 h following injection,18F-AlF-NOTA-PRGD2 uptake in the tumor reached 4.14±1.44 and 2.80±1.18 % ID/g (t=1.910, P=0.070) with tumor/brain ratios of2.95 ± 0.61 and 5.21 ± 2.62, respectively (t=-1.686, P=0.167). Both PET/CT and microPET/CT were capable of showing theradioactivity biodistribution of 18F-AlF-NOTA-PRGD2 in the mouse model and clearly displayed the tumor, but microPET/CTshowed a much better image quality. Conclusion 18F-AlF-NOTA-PRGD2 prepared by one-step radiosynthesis can selectivelytarget to the tumor, demonstrating its potential as a good radiotracer for tumor imaging.
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https://www.j-smu.com/EN/Y2014/V34/I01/51