☆ 4.7 Article

18F-labeled flavones for in vivo imaging of β-amyloid plaques in Alzheimer's brains

BIOORGANIC & MEDICINAL CHEMISTRY (2009)

期刊

BIOORGANIC & MEDICINAL CHEMISTRY

卷 17, 期 5, 页码 2069-2076

出版社

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmc.2009.01.025

关键词

Alzheimer's disease; beta-Amyloid plaque; PET; Flavone

类别

Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic

资金

Industrial Technology Research
New Energy and Industrial Technology Development Organization (NEDO) of Japan
National Institute of Biomedical Innovation (NIBIO)

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Protocol

Reagent

摘要

In vivo imaging of beta-amyloid (Ab) aggregates in the brain may lead to early detection of Alzheimer's disease (AD) and monitoring of the progression and effectiveness of treatment. The purpose of this study was to develop novel F-18-labeled amyloid-imaging probes based on flavones as a core structure. Fluoropegylated (FPEG) flavone derivatives were designed and synthesized. The affinity of the derivatives for A beta aggregates varied from 5 to 321 nM. In brain sections of AD model mice, FPEG. avones with the dimethylamino group intensely stained beta-amyloid plaques. In biodistrubution experiments using normal mice, they displayed high uptake in the brain ranging from 2.9 to 4.2% ID/g at 2 min postinjection. The radioactivity washed out from the brain rapidly (1.3-2.0% ID/g at 30 min), which is highly desirable for beta-amyloid imaging agents. FPEG. avones may be potential PET imaging agents for beta-amyloid plaques in Alzheimer's brains. (C) 2009 Elsevier Ltd. All rights reserved.

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