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Sadahiro Naka,Toshimitsu Watanabe,Yasukazu Kanai,Tadashi Watabe,Tatsumi Mitsuaki,Kato Hiroki,Shimosegawa Eku,Jun Hatazawa 대한핵의학회 2022 핵의학 분자영상 Vol.56 No.2
Purpose 4-Borono-2-[18F]fluoro-L-phenylalanine ([18F]FBPA) synthesized with [18F]F2, produced using the 18O(p, n)18F reaction, has been reported for increasing radioactivity. However, a dedicated system and complex procedure is required to reuse the costly [18O]O2 gas; also, the use of [18F]F2 as a labeling agent reduces the labeling rate and radiochemical purity.We developed a stable and practical method for [18F]FBPA synthesis by combining [18F]F2, produced using a [18O]O2 single-use system, and a [18F]CH3COOF labeling agent. Methods The produced [18F]F2 was optimized, and then [18F]FBPA was synthesized. For passivation of the target box, 0.5% F2 was pre-irradiated in argon.Gaseous products were discarded; the target box was filledwith [18O]O2 gas, and then irradiated (first irradiation). Then, the [18O]O2 gas was discarded, 0.05–0.08% F2 in argon was fed into the target box, and it was again irradiated (second irradiation). The [18F]F2 obtained after this was passed through a CH3COONa column, converting it into the [18F]CH3COOF labeling agent, which was then used for [18F]FBPA synthesis. Results The mean amount of as-obtained [18F]F2 was 55.0 ± 3.3 GBq and that of as-obtained [18F]CH3COOF was 21.6 ± 1.4 GBq after the bombardment. The radioactivity and the radiochemical yield based on [18F]F2 of [18F]FBPA were 4.72 ± 0.34 GBq and 12.2 ± 0.1%, respectively. The radiochemical purity and molar activity were 99.3 ± 0.1% and 231 ± 22 GBq/mmol, respectively. Conclusion We developed a method for [18F]FBPA production, which is more stable and practical compared with the method using [18O]O2 gas-recycling and [18F]F2 labeling agent.
Shuichi Hiroyama,Keiko Matsunaga,Miwa Ito,Hitoshi Iimori,Ippei Morita,Jun Nakamura,Eku Shimosegawa,Kohji Abe 대한핵의학회 2023 핵의학 분자영상 Vol.57 No.4
Purpose Integrin αv is a key regulator in the pathophysiology of hepatic fibrosis. In this study, we evaluated the potentialutility of an integrin αvβ3 positron emission tomography (PET) radiotracer, 18F-labeled cyclic arginine-glycine-aspartic acidpenta-peptide ([18F]F-FPP-RGD2), for detecting hepatic integrin αv and function in nonalcoholic steatohepatitis (NASH)model rats using integrin αv siRNA. Methods NASH model rats were produced by feeding a choline-deficient, low-methionine, high-fat diet for 8 weeks. PET/computerized tomography imaging and quantification of integrin αv protein, serum aspartate aminotransferase, and alanineaminotransferase were performed 1 week after single intravenous injection of integrin αv siRNA. Results Integrin αv siRNA (0.1 and 0.5 mg/kg) dose-dependently decreased hepatic integrin αv protein concentrations incontrol and NASH model rats. The hepatic mean standard uptake value of [18F]F-FPP-RGD2 was decreased dose-dependentlyby integrin αv siRNA. The mean standard uptake value was positively correlated with integrin αv protein levels in controland NASH model rats. Serum aspartate aminotransferase and alanine aminotransferase concentrations were also decreasedby siRNA injection and correlated with liver integrin αv protein expression levels in NASH model rats. Conclusion This study suggests that [18F]F-FPP-RGD2 PET imaging is a promising radiotracer for monitoring hepatic integrinαv protein levels and hepatic function in NASH pathology.