Synthesis and evaluation of novel chalcone derivatives with (99m)Tc/Re complexes as potential probes for detection of β-amyloid plaques.
Four (99m)Tc-labeled chalcone derivatives and their corresponding rhenium analogues were tested as potential probes for imaging β-amyloid plaques. The chalcones showed higher affinity for Aβ(1-42) aggregates than did (99m)Tc complexes. In sections of brain tissue from an animal model of AD, the four Re chalcones intensely stained β-amyloid plaques. In biodistribution experiments using normal mice, (99m)Tc-BAT-chalcone ([(99m)Tc]17) displayed high uptake in the brain (1.48% ID/g) at 2 min postinjection. The radioactivity washed out from the brain rapidly (0.17% ID/g at 60 min), a highly desirable feature for an imaging agent. [(99m)Tc]17 may be a potential probe for imaging β-amyloid plaques in Alzheimer's brains.
Graduate School of Biomedical Sciences, Nagasaki University, 1-4 Bunkyo-machi, Nagasaki 852-8521, Japan; Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan. morio@nagasaki-u.ac.jp
Masahiro
M
Ono
Ryoichi
R
Ikeoka
Hiroyuki
H
Watanabe
Hiroyuki
H
Kimura
Takeshi
T
Fuchigami
Mamoru
M
Haratake
Hideo
H
Saji
Morio
M
Nakayama
D000544:Alzheimer Disease / Q000000981:diagnostic imaging / Q000378:metabolism / Q000473:pathology; D016229:Amyloid beta-Peptides / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism / Q000473:pathology; D002599:Chalcone / Q000138:chemical synthesis*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005260:Female; D051379:Mice; D008822:Mice, Transgenic; D058225:Plaque, Amyloid / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000473:pathology; D011877:Radionuclide Imaging; D013667:Technetium / Q000737:chemistry; D014018:Tissue Distribution / Q000502:physiology
D016229:Amyloid beta-Peptides; D002599:Chalcone; D013667:Technetium