@article{oai:nagasaki-u.repo.nii.ac.jp:00005624,
 author = {Fuchigami, Takeshi and Yamashita, Yuki and Haratake, Mamoru and Ono, Masahiro and Yoshida, Sakura and Nakayama, Morio},
 issue = {9},
 journal = {Bioorganic & Medicinal Chemistry},
 month = {May},
 note = {We report radioiodinated chalcone derivatives as new SPECT imaging probes for amyloid β (Aβ) plaques. The monoethyleneoxy derivative 2 and allyloxy derivative 8 showed a high affinity for Aβ(1-42) aggregates with Ki values of 24 and 4.5 nM, respectively. Fluorescent imaging demonstrated that 2 and 8 clearly stained thioflavin-S positive Aβ plaques in the brain sections of Tg2576 transgenic mice. In vitro autoradiography revealed that [125I]2 displayed no clear accumulation toward Aβ plaques in the brain sections of Tg2576 mice, whereas the accumulation pattern of [125I]8 matched with the presence of Aβ plaques both in the brain sections of Tg2576 mice and an AD patient. In biodistribution studies using normal mice, [125I]2 showed preferable in vivo pharmacokinetics (4.82%ID/g at 2 min and 0.45%ID/g at 60 min), while [125I]8 showed only a modest brain uptake (1.62%ID/g at 2 min) with slow clearance (0.56%ID/g at 60 min). [125I]8 showed prospective binding properties for Aβ plaques, although further structural modifications are needed to improve the blood brain barrier permeability and washout from brain., Bioorganic & Medicinal Chemistry, 22(9), pp.2622-2628; 2014},
 pages = {2622--2628},
 title = {Synthesis and evaluation of ethyleneoxylated and allyloxylated chalcone derivatives for imaging of amyloid β plaques by SPECT},
 volume = {22},
 year = {2014}
}