<sup>18</sup>F-FLT的制备及其microPET显像

¹⁸F-FLT的制备及其microPET显像

摘要: 摘要本文制备了增殖显像剂18F-FLT，考察其稳定性及研究其在肿瘤模型鼠的microPET显像。本文以3-N-t-叔丁氧羰基-1-5’-O-(4,4’-二甲氧基三苯甲基)-2’-脱氧-3’-O-(4-硝基苯磺酰基-β-1)-苏戊呋喃糖胸腺嘧啶脱氧核苷(N-BOC-FLT)为标记前体进行氟代亲核置换反应，用HPLC检测放射化学纯度（RCP），进行稳定性研究和正常小鼠体内分布试验和肿瘤模型鼠microPET显像；研究结果显示RCP〉95%，6h内稳定，正常小鼠体内分布显示，在60min时，肾，脾，肠摄取较多，心，肝，肺，膀胱摄取次之；肿瘤模型鼠microPET显像能够清晰地观察到接种部位的放射性浓聚。

Abstract: Abstract Synthesis，stability study and MicroPET image of proliferation imaging agent 3’-deoxy-3’-18F fluorothymidine（18F-FLT）were reported. Nucleophilic substitution of fluoro replacement reaction was proceeded with N-BOC-FLT as labeling precursor. Radiochemical purity(RCP)was determined by high pressure liquid chromatography(HPLC)．Biodistribufion was performed in mice． RCP determined by HPLC was over 95％ and were stable within 6 h. Biodistribufion studies in mice showed that the uptake of 18F-FLT in kidney, spleen and intestine was higher than that of 18F-FLT in heart, liver, lung and bladder at 60min postinjection. MicroPET image of tumor in nude mice bearing tumor xenografts was clear.