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目的:制备n 68Ga－成纤维细胞活化蛋白抑制剂(FAPI)－04，进行实验研究及健康志愿者PET/CT显像，探讨其临床转化价值。n 方法:手工标记n 68Ga－FAPI－04，进行标记率、放化纯及体内外稳定性检测。取ICR小鼠16只，于注射n 68Ga－FAPI－04 1.11 MBq后5、30、60和120 min分别处死(每个时间点4只)，获得主要器官的放射性计数，计算每克组织百分注射剂量率(%ID/g)。另取3只ICR小鼠，于注射n 68Ga－FAPI－04后行microPET动态显像，观察药物在正常小鼠体内的药代动力学特性。利用HepG2人肝细胞肝癌动物模型观察肿瘤对n 68Ga－FAPI－04摄取情况。予2名健康志愿者(男女各1名，年龄分别为64岁、56岁)注射n 68Ga－FAPI－04后行PET/CT摇篮床动态显像，观察体内n 68Ga－FAPI－04分布情况。n 结果:68Ga－FAPI－04手工合成需时约20 min，放化产率为(68.7±4.0)%(经衰变校正)，放化纯>99%。室温放置180 min及血样中放置90 min，测定放化纯仍>99%。ICR小鼠体内生物学分布及microPET显像均提示n 68Ga－FAPI－04主要通过泌尿系统排泄，其余器官放射性摄取较低。荷HepG2瘤裸鼠microPET显像示肿瘤显像清晰，35 min时肿瘤与肝的靶本底比值(TBR)为2.14±0.01。健康志愿者PET/CT显像表明n 68Ga－FAPI－04在体内清除迅速。n 结论:68Ga－FAPI－04合成工艺简单，质量控制合格，动物实验结果及健康志愿者显像良好，是一种非常有应用前景的成纤维细胞活化蛋白(FAP)显像剂。n “,”Objective:To prepare n 68Ga-fibroblast activation protein inhibitor (FAPI)-04, and evaluate its biodistribution and imaging characteristics in animals and healthy volunteers, in order to investigate the clinical translation potential.n Methods:68Ga-FAPI-04 was synthesized by a manual method and its radiolabeling yield, radiochemical purity, and stability (n in vivo and n in vitro) were analyzed. ICR mice (n n=16) were scarified at 5, 30, 60 and 120 min postinjection of n 68Ga-FAPI-04 (1.11 MBq) to measure radioactive counts in main organs. The dynamic mircoPET imaging was acquired for 60 min on 3 ICR mice, and tumor imaging capabilities were examined with nude mice bearing HepG2 tumors. Furthermore, 2 healthy volunteers (1 male with age of 64 years, 1 female with age of 56 years) were recruited for the investigation of probe biodistribution in humans. A serial whole-body dynamic PET/CT scan was performed immediately following injection.n Results:68Ga-FAPI-04 was synthesized within 20 min with the radiochemical yield of (68.7±4.0)% (decay corrected). The radiochemical purities of n 68Ga-FAPI-04 were over 99% and the products were stable for 180 min n in vitro and for 90 min in blood. n 68Ga-FAPI-04 was mainly cleared through urinary tracts, while other organs only showed mild tracer accumulation. MicroPET imaging showed high uptake of n 68Ga-FAPI-04 in the tumor tissue of mice, and the ratio of tumor/liver was 2.14±0.01 (35 min). The PET/CT imaging results of healthy volunteers revealed n 68Ga-FAPI-04 could be quickly cleared.n Conclusion:68Ga-FAPI-04 has many advantages for PET imaging, such as easy labeling, good stability, quick clearance and low background signals in the liver, which can be used as an attractive PET tracer for detection hepatocellular carcinoma.n