何山震, 王淑侠, 胡孔珍, 姚保国, 唐刚华. 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J. 药学学报, 2015,50(5): 565-568.
引用本文: 何山震, 王淑侠, 胡孔珍, 姚保国, 唐刚华. 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J. 药学学报, 2015,50(5): 565-568.
HE Shan-zhen, WANG Shu-xia, HU Kong-zhen, YAO Bao-guo, TANG Gang-hua. Radiosynthesis and preliminary evaluation of 5-(11Cmethyloxy)-L-tryptophan as PET tumor imagingJ. Acta Pharmaceutica Sinica, 2015,50(5): 565-568.
Citation: HE Shan-zhen, WANG Shu-xia, HU Kong-zhen, YAO Bao-guo, TANG Gang-hua. Radiosynthesis and preliminary evaluation of 5-(11Cmethyloxy)-L-tryptophan as PET tumor imagingJ. Acta Pharmaceutica Sinica, 2015,50(5): 565-568.

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-(11Cmethyloxy)-L-tryptophan as PET tumor imaging

  • 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 (microPET) 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。

     

    Abstract: The PET tracer 5-(11Cmethyloxy)-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 microPET imaging of 5-11CMTP 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 5-11CMTP 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 5-11CMTP will be a potential amino acid tracer for tumors imaging with PET.

     

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