作为β-淀粉样蛋白斑块探针的联苯三烯的合成。
Synthesis of biphenyltrienes as probes for beta-amyloid plaques.
作者信息
Zhuang Zhi-Ping, Kung Mei-Ping, Kung Hank F
机构信息
Department of Radiology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.
出版信息
J Med Chem. 2006 May 4;49(9):2841-4. doi: 10.1021/jm051020k.
Abstract
We report a series of p-hydroxy-, p-amino-, p-monomethylamino-, and p-monofluoroethylamino-substituted biphenyltrienes that displayed high binding affinities to beta-amyloid plaques. In an in vitro binding assay using postmortem brain homogenates of Alzheimer's patients and [(125)I]9, the triene compounds showed excellent binding affinities. When labeled with suitable radionuclides, they are useful as in vivo imaging agents for detecting Abeta plaques in the brains of Alzheimer's patients.
摘要
我们报告了一系列对羟基、对氨基、对单甲基氨基和对单氟乙基氨基取代的联苯三烯，它们对β-淀粉样蛋白斑块显示出高结合亲和力。在使用阿尔茨海默病患者死后脑匀浆和[(125)I]9进行的体外结合试验中，这些三烯化合物表现出优异的结合亲和力。当用合适的放射性核素标记时，它们可用作体内成像剂，用于检测阿尔茨海默病患者大脑中的Aβ斑块。
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