Abstract
Four (99m)Tc-labeled dibenzylideneacetone derivatives and corresponding rhenium complexes were successfully synthesized and biologically evaluated as potential imaging probes for Aβ plaques using SPECT. All rhenium complexes (5a-d) showed affinity for Aβ(1-42) aggregates (Ki = 13.6-120.9 nM), and selectively stained the Aβ plaques on brain sections of transgenic mice. Biodistribution in normal mice revealed that [(99m)Tc]5a-d exhibited moderate initial uptake (0.31%-0.49% ID/g at 2 min) and reasonable brain washout at 60 min post-injection. Although additional optimizations are still needed to facilitate it's penetration through BBB, the present results indicate that [(99m)Tc]5a may be a potential SPECT probe for imaging Aβ plaques in Alzheimer's brains.
Copyright © 2013 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amyloid beta-Peptides / chemistry
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Amyloid beta-Peptides / metabolism
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Animals
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Butanones / chemistry*
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Disease Models, Animal
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Fluorescent Dyes / chemical synthesis
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Fluorescent Dyes / chemistry*
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Male
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Mice
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Mice, Inbred C57BL
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Mice, Inbred ICR
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Mice, Transgenic
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Molecular Imaging
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Molecular Structure
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Organometallic Compounds / chemical synthesis
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Organometallic Compounds / chemistry*
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Peptide Fragments / chemistry
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Peptide Fragments / metabolism
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Plaque, Amyloid / chemistry*
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Plaque, Amyloid / metabolism
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Rhenium / chemistry
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Staining and Labeling*
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Technetium / chemistry*
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Tomography, Emission-Computed, Single-Photon
Substances
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Amyloid beta-Peptides
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Butanones
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Fluorescent Dyes
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Organometallic Compounds
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Peptide Fragments
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amyloid beta-protein (1-42)
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Rhenium
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Technetium
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benzylideneacetone