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目的:制备探针n N-n 18F-氟乙基-托法替尼，探讨其用于类风湿关节炎(RA)诊疗的可行性。n 方法:采用“两步法”对托法替尼进行n 18F-氟乙基修饰，应用高效液相色谱(HPLC)对探针的标记率和放化纯进行测定，并考察探针的体内外稳定性。BABL/c小鼠(正常组；n n＝3)和胶原诱导型关节炎(CIA)模型鼠(实验组；n n＝3)注射n N-n 18F-氟乙基-托法替尼，另设阻断组(CIA模型鼠注射托法替尼+n N-n 18F-氟乙基-托法替尼；n n＝3)，3组小鼠行microPET显像，观察关节炎性反应部位对n N-n 18F-氟乙基-托法替尼的摄取情况，计算每克组织百分注射剂量率(%ID/g)及关节/肌肉(T/M)比值。采用单因素方差分析和最小显著差异n t检验分析数据。n 结果:N-n 18F-氟乙基-托法替尼的合成时间约为120 min，产率约1%，比活度>13.6 GBq/μmol，放化纯>99%。探针在PBS、血浆和体内温育2 h后，放化纯仍大于95%。MicroPET显像示，注射后30 min，n N-n 18F-氟乙基-托法替尼在CIA模型鼠关节部位的摄取高于正常组和阻断组[(10.22±1.64)、(2.71±0.26)和(2.81±0.33) %ID/g；n F＝58.26, n t值：7.83、7.67, n P值：0.001、0.002]；T/M比值也高于正常组和阻断组(24.73±5.77、2.75±1.36和2.89±0.54；n F＝40.64, n t值：6.42、6.53, n P值：0.003、0.003)。n 结论:成功制备了探针n N-n 18F-氟乙基-托法替尼，其体内外稳定性佳，体内显像性能良好，具有较好的临床应用前景。n “,”Objective:To synthesize n N-n 18F-fluoroethyl-tofacitinib, and explore its feasibility in the diagnosis of rheumatoid arthritis (RA).n Methods:The “ two-step method” was used to modify tofacitinib with n 18F-fluoroethyl, and the labeling rate and radiochemical purity of the probe were measured by high performance liquid chromatography (HPLC), and the stabilities of the probe n in vivo and n in vitro were investigated. BALB/c mice (normal group; n n=3) and collagen-induced arthritis (CIA) model mice (CIA group; n n=3) were injected with n N-n 18F-fluoroethyl-tofacitinib and CIA model mice injected with tofacitirrib and n N-n 18F-fluoroethyl-tofacitinib were as blocking group (n n=3). All mice underwent microPET imaging and the percentage injection dose per gram of tissue (%ID/g) and the uptake ratio of inflamed joints to muscle (T/M) were calculated. One-way analysis of variance and the least significant difference (LSD) n t test were used to analyze the data.n Results:The synthesis time of n N-n 18F-fluoroethyl-tofacitinib was about 120 min, with the yield approximately 1%, the specific activity >13.6 GBq/μmol, and the radiochemical purity >99%. After the probe incubated with PBS, plasma or n in vivo for 2 h, the radiochemical purity was still more than 95%. MicroPET imaging showed that 30 min after injection, the uptake of n N-n 18F-fluoroethyl-tofacitinib in the inflamed joints of CIA group was higher than that of normal group and blocking group ((10.22±1.64), (2.71±0.26) and (2.81±0.33) %ID/g; n F=58.26, n t values: 7.83, 7.67, n P values: 0.001, 0.002). The T/M of CIA group was also higher than that of normal group and blocking group (24.73±5.77, 2.75±1.36 and 2.89±0.54; n F=40.64, n t values: 6.42, 6.53, n P values: 0.003, 0.003).n Conclusions:N-n 18F-fluoroethyl-tofacitinib is successfully prepared and it is stable n in vitro with good imaging performance n in vivo. It may be used in clinic for the diagnosis of RA.n