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AbstractAbstract
[en] Objective: To evaluate the automatic synthesis of 18F-labeled cyclic RGD peptide c(RGDyK)and its biological distribution in the tumor-bearing mice. Methods: N-succinimidyl-4-18F-fluorobenzoate (18F-SFB) was automatically synthesized and then re-dissolved in acetonitrile (MeCN). The cyclic RGD peptide c(RGDyK) was mixed with an hydrous DMSO and N, N-diisopropyl ethylamine (DIPEA). 18F-FBRGD was obtained by the reaction of peptide solution with 18 F-SFB. The final product was purified by HPLC gradient separation system and solid-phase extraction method. The biodistribution study and competition test of N-4-18F-fluorobenzoyl-RGD (18F-FB-RGD) in the tumor-bearing mice was performed. Results: The labeling yield of 18F-FB-RGD was (33.6±3.5)%. The synthesis time was 110 min. The radiochemical purity was more than 98%. The tumor uptake of 18F-FB-RGD was (3.43±0.15), (2.61±0.14), (2.11±0.13), and (1.79±0.18) %ID/g, respectively, at 30, 60, 90 and 120 min after injection. The ratio of tumor to muscle activity ranged from 4.26±0.69 to 5.80±0.78. The tumor uptake decreased dramatically after RGD blockage. The uptake was (0.46±0.21) %ID/g and (2.87±0.59) %ID/g in the blocked and unblocked mice, respectively, at 60 min after blockage. Conclusions: 18F-FB-RGD can be automatically synthesized and it may become a promising tumor imaging agent. (authors)
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1 figs., 1 tabs., 13 refs.
Record Type
Journal Article
Journal
Chinese Journal of Nuclear Medicine; ISSN 0253-9780; ; v. 31(1); p. 50-53
Country of publication
ANIMALS, BETA DECAY RADIOISOTOPES, BETA-PLUS DECAY RADIOISOTOPES, DISEASES, DRUGS, FLUORINE ISOTOPES, HOURS LIVING RADIOISOTOPES, INTAKE, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, LABELLED COMPOUNDS, LIGHT NUCLEI, MAMMALS, MATERIALS, NANOSECONDS LIVING RADIOISOTOPES, NITRILES, NUCLEI, ODD-ODD NUCLEI, ORGANIC COMPOUNDS, ORGANIC NITROGEN COMPOUNDS, ORGANIC SULFUR COMPOUNDS, PROTEINS, RADIOACTIVE MATERIALS, RADIOISOTOPES, RODENTS, SEPARATION PROCESSES, SULFOXIDES, SYNTHESIS, VERTEBRATES
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