Abstract |
Two (99m)Tc/Re complexes based on flavone and aurone were tested as potential probes for imaging β- amyloid plaques using single photon emission computed tomography. Both (99m)Tc-labeled derivatives showed higher affinity for Aβ(1-42) aggregates than did (99m)Tc-BAT. In sections of brain tissue from an animal model of AD, the Re- flavone derivative 9 and Re- aurone derivative 19 intensely stained β- amyloid plaques. In biodistribution experiments using normal mice, (99m)Tc-labeled flavone and aurone displayed similar radioactivity pharmacokinetics. With additional modifications to improve their brain uptake, (99m)Tc complexes based on the flavone or aurone scaffold may serve as probes for imaging cerebral β- amyloid plaques.
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Authors | Masahiro Ono, Ryoichi Ikeoka, Hiroyuki Watanabe, Hiroyuki Kimura, Takeshi Fuchigami, Mamoru Haratake, Hideo Saji, Morio Nakayama |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 20
Issue 19
Pg. 5743-8
(Oct 01 2010)
ISSN: 1464-3405 [Electronic] England |
PMID | 20797860
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2010 Elsevier Ltd. All rights reserved. |
Chemical References |
- Amyloid beta-Peptides
- Benzofurans
- Coordination Complexes
- Flavones
- Molecular Probes
- Organotechnetium Compounds
- Peptide Fragments
- Radiopharmaceuticals
- amyloid beta-protein (1-42)
- aurone
- Rhenium
- flavone
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Topics |
- Alzheimer Disease
(diagnostic imaging)
- Amyloid beta-Peptides
(chemistry, metabolism)
- Animals
- Benzofurans
(chemistry)
- Brain
(diagnostic imaging)
- Coordination Complexes
(chemistry, pharmacokinetics)
- Disease Models, Animal
- Flavones
(chemistry)
- Mice
- Molecular Probes
- Organotechnetium Compounds
(chemistry)
- Peptide Fragments
(chemistry, metabolism)
- Plaque, Amyloid
(diagnostic imaging)
- Radiopharmaceuticals
(chemistry, pharmacokinetics)
- Rhenium
(chemistry)
- Tissue Distribution
- Tomography, Emission-Computed, Single-Photon
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