【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。更多还原

【Abstract】 The PET tracer 5-([11C]methyloxy)-L-tryptophan(5-11CMTP) was prepared by nucleophilic fluorination and alkylation reaction via a two-step procedure in order to develop specific tumor probe. The biodistribution and micro PET imaging of 5-11 CMTP 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 5-11 CMTP in tumor tissue was observed. It seems that 5-11 CMTP will be a potential amino acid tracer for tumors imaging with PET.更多还原