新型Aβ斑块显像剂^(18)F-W372

A Novel Aβ-Amyloid Imaging Agent ^(18)F-W372 for Alzheimer's Disease

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-[18 F]-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。18 F-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。18 F-W372是一种潜在的脑内Aβ淀粉显像剂。

A new A-amyloid imaging agent 7-methoxy-2 （6-fluoropyridin-3-yl） imidazo [ 2, 1-b]-8-pyridinothiazol （18 F-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 659-721 PBq/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 5 min, the washout from normal brain is fast, and the brain is （0.54±0.16）%ID/g at 30 rain 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 40 rain after injection of 18F-W372. 18F-W372 may have potential as a Aβ-amyloid imaging agent for Alzheimers disease.