【摘要】 目的研究¹²⁵I-氟-碘阿糖呋喃基尿嘧啶（FIAU）的性质及在小鼠体内的生物学分布。方法利用 Iodogen 碘化标记法对氟脱氧呋喃糖尿嘧啶（FAU）进行标记,用 Sep-Pak C18反相色谱柱进行纯化;观察¹²⁵I-FIAU 的标记率、放化纯、体外稳定性及其在小鼠体内的生物学分布。结果以Iodogen 固相氧化法标记 FAU,得到¹²⁵I-FIAU,标记率为（63.12±5.01）%;产物经 Sep-Pak C18反相色谱柱纯化后放化纯为（98.60±0.52）%;¹²⁵I-FIAU 在 PBS 及人血清中37℃条件下稳定,24 h 后放化纯>95.04%。生物学分布实验表明:标记物从小鼠血液中清除迅速,用每克组织百分注射剂量率（%ID/g）表示,0.5 h 为（4.33±1.00）%ID/g,2 h 下降为（0.77±0.06）%ID/g,至24 h 时基本清除完毕;肾脏是其主要排泄器官。结论 Iodogen 固相氧化法可以进行 FAU 碘化标记,得到标记率、放化纯及稳定性较好的¹²⁵I-FIAU,该标记物主要经肾脏排泄。更多还原

【Abstract】 Objective The aim of this study was to label 2’-fluoro-2’-deoxy-1-β-D-arabinofurano- syluracil（FAU）with ¹²⁵I,and to investigate the characteristics of the labeled compound as well as its bio- distribution in mice.Methods FAU was radiolabeled with Na¹²⁵I using the Iodogen method.The Sep-Pak C18 reverse phase column was used to purify the labeled product.The labeling efficiency,radiochemical purity,the in vitro stability and its biodistribution in mice were observed.Results FAU was successfully la- beled with Na¹²⁵I with the labeling efficiency of（63.12±5.01）%.The radiochemical purity was（98.60± 0.52）%.¹²⁵I-5-iodo-FAU（FIAU）was stable in PBS and fresh human serum under 37℃ and the radio- chemical purity remained more than 95.04% after 24 h.Mouse experiment showed that the radiolabeled product was washed out from blood quickly.The uptake expressed as percentage activity of injected dose per gram of tissue（%ID/g）was（4.33±1.00）%ID/g at 0.5 h and（0.71±0.06）%ID/g at 2 h after in- jection.The ¹²⁵I-FIAU was mainly excreted through’kidney.Conclusions ¹²⁵I-FIAU could be obtained by labeling FAU with the Iodogen method with satisfactory labeling efficiency,radiochemical purity and stabili- ty.Mouse biodistribution experiment showed it was mainly excreted through kidney.更多还原