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目的 制备PET显像剂 6 18F 多巴 ( 6 18F DOPA)并研究其在大鼠体内的生物分布。方法 使用小型回旋加速器生产18F离子 ,经亲核取代、手性相转移催化烷基化等 4步反应 ,合成得到无载体的 6 18F DOPA。 2 4只SD大鼠分为 6组 ,每只经尾静脉注射 1 .1 1MBq 6 18F DOPA ,经 5,30 ,6 0 ,90 ,1 2 0和 1 50min后分别处死 ,解剖 ,取有关组织、脏器称重并测定放射性计数。结果 6 18F DOPA合成的放化产率为 3.8%～ 7.5% (衰变校正后 ) ,合成时间 1 0 0min ,放化纯度大于 99%。大鼠体内生物分布显示纹状体内有明显的放射性浓集 ,而大脑、皮质、小脑中放射性较低 ;纹状体 /小脑放射性比值在 6 0min达 5.9;其他组织器官中的放射性快速清除 ,无明显浓集。结论 建立的 6 18F DOPA合成方法有效可靠 ,6 18F DOPA主要分布在纹状体内。
Objective To prepare PET imaging agent 6 18 F DOPA and study its biodistribution in rats. Methods A small cyclotron was used to produce 18F ion. The nucleophilic substitution and chiral phase transfer catalytic alkylation were used to synthesize 18F DOPA. Twenty-four SD rats were divided into 6 groups, each of which was injected with 1.11 MBq 6 18F DOPA through the tail vein. After 5, 30, 60, 90, 120 and 150 min respectively, the rats were killed and dissected. , Organs were weighed and radioactivity was measured. Results 6 18F DOPA synthesis radiochemical yield of 3.8% to 7.5% (after decay correction), the synthesis time of 100min, radiochemical purity greater than 99%. The biodistribution of the striatum showed obvious radioactive concentration in the striatum, but lower in the cerebrum, cortex and cerebellum. The radioactivity ratio of striatum to cerebellum reached 5.9 at 60 min. The radioactivity in other tissues and organs was rapidly cleared without Obviously concentrated. Conclusion The established 6 18F DOPA synthesis method is effective and reliable, 6 18F DOPA is mainly distributed in the striatum.