99mTc/Re complexes based on flavone and aurone as SPECT probes for imaging cerebral β-amyloid plaques.
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.
Ono
Masahiro
M
Graduate School of Biomedical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan. ono@pharm.kyoto-u.ac.jp
Ikeoka
Ryoichi
R
Watanabe
Hiroyuki
H
Kimura
Hiroyuki
H
Fuchigami
Takeshi
T
Haratake
Mamoru
M
Saji
Hideo
H
Nakayama
Morio
M
D000544:Alzheimer Disease / Q000000981:diagnostic imaging; D016229:Amyloid beta-Peptides / Q000737:chemistry / Q000378:metabolism; D000818:Animals; D001572:Benzofurans / Q000737:chemistry*; D001921:Brain / Q000000981:diagnostic imaging*; D056831:Coordination Complexes / Q000737:chemistry* / Q000493:pharmacokinetics; D004195:Disease Models, Animal; D047309:Flavones / Q000737:chemistry*; D051379:Mice; D015335:Molecular Probes; D015609:Organotechnetium Compounds / Q000737:chemistry*; D010446:Peptide Fragments / Q000737:chemistry / Q000378:metabolism; D058225:Plaque, Amyloid / Q000000981:diagnostic imaging*; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000493:pharmacokinetics; D012211:Rhenium / Q000737:chemistry*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon
D016229:Amyloid beta-Peptides; D001572:Benzofurans; D056831:Coordination Complexes; D047309:Flavones; D015335:Molecular Probes; D015609:Organotechnetium Compounds; D010446:Peptide Fragments; D019275:Radiopharmaceuticals; C075222:amyloid beta-protein (1-42); C486837:aurone; D012211:Rhenium; C043562:flavone