目的 研制合成5-(18F-3-氟丙氧基)-L-色氨酸(5-18FPTP)的有效方法,并进行动物体内生物分布实验,应用动物模型评价其区分炎症与肿瘤的价值。方法 采用亲核取代反应,经两步法合成5-18FPTP。各组动物小鼠分别在给药后按规定的不同时间处死,测定各器官的摄取率,得到小鼠各器官的5-18FPTP生物分布。对2只炎症-肿瘤模型小鼠给药后60 min进行5-18FPTP的正电子发射断层(PET)显像,分析炎症、肿瘤对5-18FPTP的摄取情况。 结果 5-18FPTP的标记时间约为60 min,未校正的总放射化学产率为(21±4.6)%,放射化学纯度大于95%。正常小鼠生物分布和PET肿瘤-炎症模型显像显示,肝、肾、血等脏器摄取较高且滞留时间较长,脑及肌肉摄取较低,肿瘤组织可以有效摄取5-18FPTP,而炎症组织几乎不摄取5-18FPTP。结论 5-18FPTP标记简单,能够有效区分肿瘤和炎症组织,有望成为特异性的肿瘤氨基酸代谢的正电子药物。
Abstract
ObjectiveTo develop 5-(3-fluoropropyloxy)-L-tryptophan(5-18FPTP)as a new amino acid positron emission tomography (PET) tracer for the differentiation of tumor and inflammation. Methods 5-18FPTP was prepared by nucleophilic fluorination and alkylation reaction via a two-step procedure. Twenty mice were divided into five groups randomly and the biodistribution of 5-18FPTP in normal mice was determined at different time after injecting the tracer by tail vein. Also, two mice bearing tumor and inflammation received PET imaging at 60 min after injecting the tracer to detect the uptake of the tracer in tumor and inflammatory tissue. Results The overall synthesis time of 5-18FPTP was about 60 min, the overall radiochemical yield with no decay correction was (21?4.6)%, and the radiochemical purity was more than 95%. High uptake and long retention time of 5-18FPTP in liver, kidney and blood were observed. But low uptake in brain and muscle were found. Furthermore, high uptake of 5-18FPTP in tumor but almost no uptake of 5-18FPTP in inflammatory tissue were observed. Conclusion 5-18FPTP is easy to prepare and can be used to differentiate tumors and inflammatory tissues. It seems to be a potential amino acid tracer for tumor imaging with PET.
关键词
5-(18F-3-氟丙氧基)-L-色氨酸(5-18FPTP) /
合成 /
PET显像
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Key words
L-5-(3- fluoropropyloxy)tryptophan (5-18FPTP) /
synthesis /
PET imaging
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中图分类号：
R817
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参考文献
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脚注
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基金
国家高科技计划(863计划)专题课题(2008AA02Z430);国家自然科学基金面上项目(30970856);中山大学百人计划引进人才科研启动基金项目(80000-3171313);广东省科技计划项目(2010B031600054);广州市科技计划重点项目(2011J5200025);教育部留学回国启动基金(教外司留609号);广东省医学科研基金(A2011035)
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