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Synthesis of 18F-FP-Lladtthhrpwt as a new probe for the detection of lung cancer by microPET

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Author:
No author available
Journal Title:
Chinese Journal of Nuclear Medicine and Molecular Imaging
Issue:
2
DOI:
10.3760/cma.j.issn.2095-2848.2014.02.013
Key Word:
肺肿瘤;肽类;氟放射性同位素;化学合成;放射性核素显像;小鼠,裸;Lung neoplasms;Peptides;Fluorine radioisotopes;Chemical synthesis;Radionuclide imaging;Mice,nude

Abstract: Objective To prepare 18F-2-fluoropropionyl (FP)-Lladtthhrpwt (18 F-FP-ZS-6) by a multifunctional 18F radiolabeling module and investigate its in vivo distribution in human lung cancer cell (NCI-H1299)-bearing nude mice by microPET.Methods Using a phage display peptide library to screen and identify Lladtthhrpwt (ZS-6) which has an affinity for human lung cancer.PET-MF-2V-IT-I synthesizer was used for the synthesis and purification of 18F-FP-ZS-6.MicroPET studies were carried out in NCI-H1299-bearing nude mice after injection of 18F-FP-ZS-6.Results 4-nitrophenyl 2-[18F] fluoropropionate (18F-NFP) was prepared by " one-pot" radiochemical procedure.The radiochemical yield of 18F-FP-ZS-6 was (5±2)% (n=3,decay-corrected) from 18F and the radiochemical purity was more than 95%.MicroPET studies showed that the uptake of 18F-FP-ZS-6 was high in the tumor and stomach of NCI-H1299-bearing nude mice model.The tumor uptake of 18F-FP-ZS-6 was 0.329,0.350,0.405,0.433,0.420,0.415,0.402,0.403,0.390 %ID/g at 5,15,25,35,45,55,65,75,85 min post-injection,respectively.The tumor uptake peak was at 35 min post-injection and then 18F-FP-ZS-6 was cleared slowly.Conclusions 18F-FP-ZS-6 could be successfully prepared.It might be a potential tracer for imaging human lung cancer.

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