【摘要】 目的:⁶⁴Cu有半衰期较长、化学反应温和的优势,本研究合成新型乏氧分子影像学探针⁶⁴Cu-ATSM,并与18F-氟硝基咪唑(¹⁸F-fluoromisonidazole,18F-FMISO)进行初步比较。方法:使用SIEMENS Eclipse HP 11 Me V小型医用回旋加速器系统,Comecer ALCEO EDL、PRF、TADDEO放射性模块和定制铂金靶盘进行64Ni电镀、⁶⁴Cu纯化和⁶⁴Cu-ATSM合成。用伽马能谱仪和高效液相色谱（high performance liquid chromatography,HPLC）进行放射核纯度、放化纯度和稳定性检测。在荷人乳腺癌MDB-MA-231模型中进行小动物PET/CT显像并与自制的¹⁸F-FMISO进行比较。结果:实现了⁶⁴Cu-ATSM的自动化生产,产率60%,放射性核纯度>99%,放化纯度>95%,标记物稳定性>6 h。与¹⁸F-FMISO一样能反映肿瘤乏氧情况,且注射1 h后T/M值即能达5.28。结论:成功用11 Me V SIEMENS回旋加速器和Comecer ALCEO模块合成了⁶⁴Cu-ATSM,荷人乳腺癌小动物PET/CT乏氧显像靶/本比高。更多还原

【Abstract】 Objective: To investigate the synthesis and application of ⁶⁴Cu-ATSM in hypoxia imaging of xenografted MDBMA-231 breast cancer. Methods: ⁶⁴CuCl₂ was prepared by SIEMENS Eclipse HP 11 Me V cyclotron, Comecer ALCEO EDL, PRF and TADDEO pharmaceutical modules, and the modified platinum target plate. And then the prepared ⁶⁴CuCl₂ and synthesized ⁶⁴CuATSM were monitored by energy spectroscopy and high performance liquid chromatography（HPLC） for detection of radioactive purity, radiochemical purity and stability. ⁶⁴Cu-ATSM was intravenously injected into MDB-MA-231 cells xenografted nude mouse and then imaged by micro PET/CT. The results were compared with that of 18F-fluoromisonidazole(¹⁸F-FMISO) injected 4 d after ⁶⁴Cu-ATSM imaging. Results: The automatic production of ⁶⁴Cu-ATSM with a productivity of 60% without radioactive and radiochemical impurity was achieved. ⁶⁴Cu-ATSM was stable at 6 h after synthesis. Both ⁶⁴Cu-ATSM and 18F-FMISO could demonstrate the hypoxic degree of MDB-MA-231 cell xenografted tumor. And the tumor/muscle（T/M） ratio of ⁶⁴Cu-ATSM was 5.28, which was significantly higher than that of ¹⁸F-FMISO（1.88）. Nevertheless, three hours after injection, the T/M ratios of the two probes were similar. Conclusion: The synthesized ⁶⁴Cu-ATSM could image the hypoxic condition of MDB-MA-231 xenografted tumor.更多还原