化学
体内
荧光
共轭体系
生物物理学
淀粉样蛋白(真菌学)
近红外光谱
阿尔茨海默病
病理
疾病
神经科学
有机化学
无机化学
生物技术
物理
生物
聚合物
医学
量子力学
作者
Hualong Fu,Mengchao Cui,Zhao Liu,Peiyu Tu,Kaixiang Zhou,Jiapei Dai,Boli Liu
标识
DOI:10.1021/acs.jmedchem.5b00861
摘要
Alzheimer's disease (AD) is pathologically characterized by the accumulation of β-amyloid (Aβ) deposits in the parenchymal and cortical brain. In this work, we designed, synthesized, and evaluated a series of near-infrared (NIR) probes with electron donor–acceptor end groups interacting through a π-conjugated system for the detection of Aβ deposits in the brain. Among these probes, 3b and 3c had excellent fluorescent properties (emission maxima > 650 nm and high quantum yields) and displayed high sensitivity and high affinities to Aβ aggregates (3b, Kd = 8.8 nM; 3c, Kd = 1.9 nM). Both 3b and 3c could readily penetrate the blood–brain barrier with high initial brain uptake and fast to moderate washout from the brain. In vivo NIR imaging revealed that 3b and 3c could efficiently differentiate transgenic and wild-type mice. In summary, our research provides new hints for developing smarter and more activatable NIR probes targeting Aβ.
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