肿瘤靶向PET探针5-(^11C-甲氧基)-L-色氨酸的合成及初步生物学评价  

Radiosynthesis and preliminary evaluation of 5-([^(11)C]methyloxy)-L-tryptophan as PET tumor imaging

作　　者：何山震[1,2] 王淑侠[1] 胡孔珍[2] 姚保国[2] 唐刚华[2] 

机构地区：[1]广东省人民医院,广东省医学科学院,广东广州510080 [2]中山大学附属第一医院,广东广州510080

出　　处：《药学学报》2015年第5期565-568,共4页Acta Pharmaceutica Sinica

基　　金：广东省企业技术研发与升级改造专项资金项目(2013B021800191);广东省医学科研基金资助项目(A2011035)

摘　　要：本文采用11CH3-triflate甲基化的方法设计合成了新型的氨基酸类PET探针5-(11C-甲氧基)-L-色氨酸(5-11CMTP),并进行了5-11CMTP的小鼠生物分布和S180肿瘤模型小动物PET断层(micro PET)显像。结果表明,5-11CMTP被有效合成,未校正的总放射化学产率为(14.6±7.2)%,放射化学纯度大于95%。正常小鼠生物分布显示,肝、肾、血等摄取较高且滞留时间较长,脑及肌肉摄取较低,而S180肿瘤组织可以有效摄取5-11CMTP,有望成为特异性的肿瘤氨基酸代谢的正电子药物。The PET tracer 5-（[11C]methyloxy）-L-tryptophan （5-1~CMTP） was prepared by nucleophilic fluorination and alkylation reaction via a two-step procedure in order to develop specific tumor probe. The biodistribution and microPET imaging of 5-HCMTP were executed. The results unveiled that the overall radiochemical yield with no decay correction was （14.6 ±7.2）%, the radiochemical purity was more than 95% and high uptake and long retention time of 5-11 CMTP in liver, kidney and blood were observed but low uptake in brain and muscle were found, furthermore, high uptake of 5- 11CMTP in tumor tissue was observed. It seems that 5-11 CMTP will be a potential amino acid tracer for tumors imaging with PET.

关 键 词：5-(11C-甲氧基)-L-色氨酸 合成 PET显像 

分 类 号：TQ463[化学工程—制药化工] R817[医药卫生—影像医学与核医学]