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目的:自动化合成Aln 18F-1,4,7-三氮杂环壬烷-1,4,7-三乙酸(NOTA)-成纤维细胞激活蛋白抑制剂(FAPI)-04,并进行体内显像,评估其诊断肿瘤的效能。n 方法:利用All-in-one型自动合成模块合成Aln 18F-NOTA-FAPI-04,并进行质量分析;取3只正常BALB/c小鼠和3只4T1小鼠乳腺癌荷瘤小鼠进行PET/CT显像,观察体内Aln 18F-NOTA-FAPI-04分布情况;对1例肝细胞肝癌患者(男,51岁)进行Aln 18F-NOTA-FAPI-04和n 18F-FDG PET/CT显像,评估其对肝癌的诊断效能。n 结果:自动化合成Aln 18F-NOTA-FAPI-04的时间约为35 min,合成产率约为(25.2±1.9)%(衰减校正后,n n=3),产品为无色透明溶液,pH值为7.0~7.5,其比活度为(46.11±3.07) GBq/μmol(衰减校正后,n n=3),放化纯大于99.0%,室温放置6 h后放化纯仍大于98.0%。小鼠体内显像示Aln 18F-NOTA-FAPI-04的生理性摄取主要在胆道系统和膀胱中,且高度浓聚于肿瘤病灶区域;肝细胞肝癌患者PET/CT显像示Aln 18F-NOTA-FAPI-04和n 18F-FDG PET/CT在胸骨旁淋巴结、膈上前组淋巴结、肝门区淋巴结、胰十二指肠韧带区淋巴结、腹主动脉旁淋巴结的靶本比值(TBR)分别为4.1、8.9、5.4、4.8、2.2和1.0、2.8、5.0、2.1、1.1。n 结论:基于All-in-one型自动合成模块合成Aln 18F-NOTA-FAPI-04,合成时间较短、产率高、稳定性好,高度浓聚于病灶区域,其PET图像对比度高,诊断性能优异。n “,”Objective:To automatically synthesize Aln 18F-1, 4, 7-triazacyclononane-1, 4, 7-triacetic acid (NOTA)-fibroblast activation protein inhibitor (FAPI)-04, perform PET/CT imaging n in vivo, and evaluate its diagnostic efficacy on tumors.n Methods:Aln 18F-NOTA-FAPI-04 was produced in All-in-one automatic synthesis module and its quality control was conducted by high performance liquid chromatography (HPLC) equipped with a radioactive detector. Aln 18F-NOTA-FAPI-04 PET/CT imaging was performed in normal BALB/c mice (n n=3) and 4T1 breast cancer models (n n=3) to determine its biodistribution. Then Aln 18F-NOTA-FAPI-04 and n 18F-FDG PET/CT imaging were performed in a hepatocellular carcinoma patient (male, 51 years old).n Results:The synthesis time of Aln 18F-NOTA-FAPI-04 was about 35 min, and the radiochemical yield was (25.2±1.9)% (attenuation correction, n n=3). The product was colorless transparent solution with pH value of 7.0-7.5, and the specific activity was (46.11±3.07) GBq/μmol (attenuation correction,n n=3). The radiochemical purity was above 99.0% and was still above 98.0% at room temperature after 6 h. PET/CT imaging in mice showed that physiological uptake of Aln 18F-NOTA-FAPI-04 was mainly in biliary system and bladder, and Aln 18F-NOTA-FAPI-04 highly concentrated in tumor xenografts. PET/CT imaging in the patient showed that Aln 18F-NOTA-FAPI-04 obtained high tumor background ratio (TBR) values of 4.1, 8.9, 5.4, 4.8, 2.2 in parasternal lymph nodes, anterior diaphragmatic lymph nodes, hilar lymph nodes, pancreaticoduodenal ligament lymph nodes, abdominal aortic lymph nodes, respectively, while TBR values were 1.0, 2.8, 5.0, 2.1, 1.1 by n 18F-FDG.n Conclusions:Aln 18F-NOTA-FAPI-04 can be synthesized with short time, high radiochemical yield and good stability using All-in-one module. Aln 18F-NOTA-FAPI-04 PET/CT imaging has high contrast and excellent diagnostic efficacy on tumors.n