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Molecules 2012, 17(4), 4252-4265; doi:10.3390/molecules17044252

(E)-5-Styryl-1H-indole and (E)-6-Styrylquinoline Derivatives Serve as Probes for β-Amyloid Plaques

Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China
Authors to whom correspondence should be addressed.
Received: 20 February 2012 / Revised: 28 March 2012 / Accepted: 29 March 2012 / Published: 10 April 2012
(This article belongs to the Section Medicinal Chemistry)
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We report the synthesis and biological evaluation of novel (E)-5-styryl-1H-indole and (E)-6-styrylquinoline derivatives as probes for imaging β-amyloid (Aβ) plaques. These derivatives showed binding affinities for Aβ1–40 aggregates with Ki values varying from 4.1 to 288.4 nM. (E)-5-(4-iodostyryl)-1H-indole (8) clearly stained Aβ plaques in the brain sections of Alzheimer’s disease (AD) model mice (APP/PS1). Furthermore, autoradiography for [125I]8 displayed intense and specific labeling of Aβ plaques in the brain sections mentioned above with low background. In biodistribution experiments using normal mice [125I]8 showed high initial brain uptake followed by rapid washout (4.27 and 0.64% ID/g at 2 and 30 min post injection, respectively). These findings suggests that [123I]8 may be a potential SPECT imaging agent for detecting Aβ plaques in AD brain. View Full-Text
Keywords: Alzheimer’s disease; β-amyloid plaques; binding affinity; imaging agent; SPECT Alzheimer’s disease; β-amyloid plaques; binding affinity; imaging agent; SPECT

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Yang, Y.; Jia, H.-M.; Liu, B.-L. (E)-5-Styryl-1H-indole and (E)-6-Styrylquinoline Derivatives Serve as Probes for β-Amyloid Plaques. Molecules 2012, 17, 4252-4265.

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