新型Aβ斑块显像剂18F-W372

    A Novel Aβ-Amyloid Imaging Agent 18F-W372 for Alzheimer’s Disease

    • 摘要: 合成诊断阿尔茨海默病(Alzheimer’s disease,AD)的Aβ斑块显像剂:7-甲氧基-2(6-[18F]-氟-吡啶-3-基)咪唑[2,1-β]-8-吡啶噻唑(18F-W372),不校正合成效率为(25.3±7.1)%(n=6),产品放化纯大于99.5%,比活度为659~721PBq/mol。 18F-W372小鼠体内分布实验显示,初始5min脑摄取为(4.36±1.44)%ID/g,清除较快,30min为(0.54±0.16)%ID/g,摄取比达到8,具有良好的生物学性能。急性毒性实验表明该药物安全可靠。在体试验显示药物注射40min,AD患者平均皮层/小脑吸收显著高于健康老年对照组。18F-W372是一种潜在的脑内Aβ淀粉显像剂。

       

      Abstract: A new Aβ-amyloid imaging agent 7-methoxy-2(6-fluoropyridin-3-yl)imidazo[2,1-b]-8-pyridinothiazol (18F-W372) is synthesized, the non-decay corrected radiochemical yield is (25.3±7.1)% (n=6), the radiochemical purity is more than 99.5%, and the specific activity is 659-721PBq/mol. Biodistribution of the 18F-W372 in mice indicates that uptake is high in brain, the brain is (4.36±1.44)%ID/g at 5min, the washout from normal brain is fast, and the brain is (0.54±0.16)%ID/g at 30min post injection. The acute toxicity test of 18F-W372 proves its safety in clinical use. The cortical/cerebellar specific uptake is higher in AD patients than in controls at 40min after injection of 18F-W372. 18F-W372 may have potential as a Aβ-amyloid imaging agent for Alzheimer’s disease.

       

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