唐刚华, 王明芳, 唐小兰, 罗磊, 甘满权. S-(2-18F-氟代乙基)-L-蛋氨酸的合成及其放射药理活性J. 药学学报, 2003, 38(12): 915-918.
引用本文: 唐刚华, 王明芳, 唐小兰, 罗磊, 甘满权. S-(2-18F-氟代乙基)-L-蛋氨酸的合成及其放射药理活性J. 药学学报, 2003, 38(12): 915-918.
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TANG Gang-hua, WANG Ming-fang, TANG Xiao-lan, LUO Lei, GAN Man-quan. Synthesis and radiopharmacology of S-(2-18F-fluoroethyl)-L-methionine for tumor imagingJ. Acta Pharmaceutica Sinica, 2003, 38(12): 915-918.
Citation: TANG Gang-hua, WANG Ming-fang, TANG Xiao-lan, LUO Lei, GAN Man-quan. Synthesis and radiopharmacology of S-(2-18F-fluoroethyl)-L-methionine for tumor imagingJ. Acta Pharmaceutica Sinica, 2003, 38(12): 915-918.
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S-(2-18F-氟代乙基)-L-蛋氨酸的合成及其放射药理活性

Synthesis and radiopharmacology of S-(2-18F-fluoroethyl)-L-methionine for tumor imaging

    摘要
  • 摘要: 目的研制肿瘤氨基酸代谢显像剂S-(2-18F-氟代乙基)-L-蛋氨酸(18FEMET),评价其区分炎症和肿瘤的价值。方法采用亲核取代反应,由两步法合成18FEMET。测定正常小鼠、肿瘤及炎症小鼠体内FEMET生物分布,对模型小鼠进行18FEMET PET显像,并与2-18F-2-脱氧-D-葡萄糖(FDG)和O-(2-18F-氟代乙基)-L-酪氨酸(FET)比较。结果18FEMET手工合成时间约为70 min,未校正总放化产率为15%～25%,放化纯度大于95%。正常小鼠中胰腺、肾脏、结肠、肝和心脏等脏器摄取18FEMET较高,且放射性滞留时间较长,血液和脑摄取18FEMET较低。肿瘤细胞可高度摄取18FEMET,FDG和FET,炎症组织也可高度摄取FDG,但几乎不摄取18FEMET和FET。结论18FEMET制备简便,能够区分肿瘤和炎症,可望成为一种有前景的特异性肿瘤氨基酸代谢PET显像剂。

     

    Abstract: AimTo develop S-(2-18F-fluoroethyl)-L-methionine (18FEMET) as an amino acid positron emission tomography (PET) tracer for tumors, and to evaluate the value of 18FEMET in the differentiation of experimental tumor and experimental inflammation. Methods18FEMET was prepared by nucleophilic fluorination reaction via a two-step procedure. Biodistribution of 18FEMET in normal mice, carcinoma-bearing mice and inflammatory mice, and 18FEMET PET imaging for carcinoma-bearing mice and inflammatory mice were performed compared with 2-［18F］fluoro-2-deoxy-D-glucose (FDG) and O-(2-［18F］fluoroethyl)-L-tyrosine (FET). ResultsThe overall radiochemical yield with no decay correction was 15%-25%, the whole synthesis time was about 70 min by manual operation, and the radiochemical purity was above 95%. High uptake and long retention of 18FEMET in pancreas, kidney, colon, liver and heart were observed. But low uptakes in brain and blood were found. Furthermore, high uptake of 18FEMET, FDG and FET in tumor, high uptake of FDG in inflammatory tissue, and almost no uptake of 18FEMET and FET in inflammatory tissue were also observed. Conclusion18FEMET is easy to prepare and can be used to differentiate between tumor and inflammatory tissue. It seems to be a potential amino acid tracer for tumors with PET imaging.

     

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