@article{oai:nagasaki-u.repo.nii.ac.jp:00015666, author = {Watanabe, Hiroyuki and Ono, Masahiro and Haratake, Mamoru and Kobashi, Nobuya and Saji, Hideo and Nakayama, Morio}, issue = {13}, journal = {Bioorganic & medicinal chemistry}, month = {May}, note = {We synthesized a novel series of phenylindole (PI) derivatives and evaluated their biological activities as probes for imaging Abeta plaques in vivo. The affinity for Abeta plaques was assessed by an in vitro-binding assay using pre-formed synthetic Abeta aggregates. 2-Phenyl-1H-indole (2-PI) derivatives showed high affinity for Abeta42 aggregates with K(i) values ranging from 4 to 32nM. 2-PI derivatives clearly stained Abeta plaques in an animal model of AD. In biodistribution experiments using normal mice, 2-PI derivatives displayed sufficient uptake for imaging, ranging from 1.1% to 2.6% ID/g. Although additional modifications are necessary to improve uptake by and clearance from the brain, 2-PI derivatives may be useful as a backbone structure to develop novel Abeta imaging agents., Bioorganic & medicinal chemistry, 18(13), pp.4740-4746; 2010}, pages = {4740--4746}, title = {Synthesis and characterization of novel phenylindoles as potential probes for imaging of beta-amyloid plaques in the brain.}, volume = {18}, year = {2010} }