【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-[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。更多还原

【Abstract】 A new Aβ-amyloid imaging agent 7-methoxy-2(6-fluoropyridin-3-yl)imidazo-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 659-721 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 min 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 min after injection of 18F-W372.18F-W372 may have potential as a Aβ-amyloid imaging agent for Alzheimer’s disease.更多还原