脑显像剂IMP的放射性碘标记及动物实验

THE PREPARATION AND ANIMAL TESTING OF 125-I-IMP AS A SCINTIGRAPHIC AGENT FOR BRAIN

  • 摘要: 文章报道了对本校合成的RS-N-Isopropyl-P-Iodoamphetamine进行~(125)I标记和动物实验的初步结果。我们采用水热法进行同位素交换反应,在Cu(II)和过量还原剂存在的条件下,可以方便地获得高标记率的~(125)I-IMP。经萃取纯化后,放化纯度>98%;游离~(125)I<1%。测定了在大鼠体内静脉注射~(125)I-IMP的分布,结果表明,~(125)I-IMP具有脑摄取率高、脑与血的比值大、在脑贮留时间长等优点,是一种有用的新型脑显象剂。

     

    Abstract: RS-N-isopropyl-p-iodoampheta (IMP) is radio-iodinated by isotopicexchange using Cu (I) as catalyst in presence of an excess of Sn (II) as reductor.The metod is simple and fast. A quantitative (99%) labelling yield of ~(125)I-IMPcan be obtained within 30 minutes. Free ionic ~(125)I<3%. After ether extraction,radiochemical purity is greater than 98%, free ionic ~(125)I<1%. For Biodistri-bution of ~(125)I-IMP in Spragne-Dawlay rat, the brain uptake is prompt, with1.32%/g of the injected dose reaching the brain by 5 min and peak uptake(1.49%/g) at 1h. There is a slight fall in brain activity after 3h. At all timesthe brain-to-blood ratio is more than 12. After the administration the highestradioactivity ratios of brain/blood, brain/skeletal muscle and brain/bone are17.5,5 and 9.at 30--60min respectively.

     

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