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- W2954328774 abstract "1061 Objectives: Based on the principle of oxime formation, the 18F labeling of polypeptides can be achieved via a reaction between an aldehyde group-containing 18F-prosthetic group and an aminooxy-modified polypeptide. The focus of this study was to investigate the one-step synthesis of 2-[18F]fluoro-2-deoxyglucose ([18F]FDG)-RGD from open-ring [18F]FDG and the aminooxy-modified RGD peptide cyclo(RGDfK)-ONH2 and to study the biological distribution of [18F]FDG-RGD in a nude mouse model of human neuroglioma. Methods: The aminooxy-modified RGD peptide cyclo(RGDfK)-ONH2 was used as the precursor to react with [18F]FDG at 100 ℃ and pH 1.5-2.5 for 30 min to synthesize [18F]FDG-RGD. The labeling rate, radiochemical purity, in vitro stability of the product were measured, and the biological distribution of [18F]FDG-RGD in tumor-bearing nude mice at 30 min, 60 min and 120 min were analyzed. Results: The labeling rate of [18F]FDG-RGD was 14.5%, the radiochemical purity was greater than 95%. [18F]FDG-RGD was mainly excreted by the kidneys, and blood clearance was rapid. One hour after injection, the radioactive uptake values for the kidney, liver, small intestine, muscle and blood were (1.95 ± 0.15)% ID/g, (0.77 ± 0.21)% ID/g, (0.64 ± 0.05)% ID/g, (0.26 ± 0.17)% ID/g and (0.42 ± 0.05)% ID/g, respectively. One hour after injection, the uptake of [18F]FDG-RGD by tumors was (1.83 ± 0.12)% ID/g, Tumor/Muscle (T/M) was 7.03 ± 0.04. Conclusion: The synthesis of [18F]FDG-RGD can be achieved via oximation. This method is simple and easy to promote. The blood clearance of [18F]FDG-RGD is rapid, its radioactive background is low, its binding to integrin αvβ3 receptor is specific, its uptake by tumors is extremely high,; therefore, [18F]FDG-RGD maybe be used for the imaging of integrin-positive tumors." @default.
- W2954328774 created "2019-07-12" @default.
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- W2954328774 date "2018-05-01" @default.
- W2954328774 modified "2023-09-24" @default.
- W2954328774 title "Synthesis and application of [18F]FDG-RGD" @default.
- W2954328774 hasPublicationYear "2018" @default.
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