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99mTc/Re complexes based on flavone and aurone as SPECT probes for imaging cerebral β-amyloid plaques.

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.
AuthorsMasahiro Ono, Ryoichi Ikeoka, Hiroyuki Watanabe, Hiroyuki Kimura, Takeshi Fuchigami, Mamoru Haratake, Hideo Saji, Morio Nakayama
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 20 Issue 19 Pg. 5743-8 (Oct 01 2010) ISSN: 1464-3405 [Electronic] England
PMID20797860 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 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
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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