1442656-92-9Relevant articles and documents
Synthesis and biological evaluation of 18F-labled 2-phenylindole derivatives as PET imaging probes for β-amyloid plaques
Fu, Hualong,Yu, Lihai,Cui, Mengchao,Zhang, Jinming,Zhang, Xiaojun,Li, Zijing,Wang, Xuedan,Jia, Jianhua,Yang, Yanping,Yu, Pingrong,Jia, Hongmei,Liu, Boli
, p. 3708 - 3714 (2013/07/27)
A novel series of fluorinated 2-phenylindole derivatives were synthesized and evaluated as β-amyloid imaging probes for PET. The in vitro inhibition assay demonstrated that their binding affinities for Aβ1-42 aggregates ranged from 28.4 to 1097.8 nM. One ligand was labeled with 18F ([18F]1a) for its high affinity (Ki = 28.4 nM), which was also confirmed by in vitro autoradiography experiments on brain sections of transgenic mouse (C57BL6, APPswe/PSEN1, 11 months old, male). In vivo biodistribution experiments in normal mice showed that this radiotracer displayed high initial uptake (5.82 ± 0.51% ID/g at 2 min) into and moderate washout (2.77 ± 0.31% ID/g at 60 min) from the brain. [ 18F]1a could be developed as a promising new PET imaging probe for Aβ plaques although necessary modifications are still needed.
