Synthesis and biological evaluation of 18F-labled 2-phenylindole derivatives as PET imaging probes for β-amyloid plaques.

Abstract:

: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 Aβ(1-42) aggregates ranged from 28.4 to 1097.8 nM. One ligand was labeled with (18)F ([(18)F]1a) for its high affinity (K(i)=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. [(18)F]1a could be developed as a promising new PET imaging probe for Aβ plaques although necessary modifications are still needed.

journal_name

Bioorg Med Chem

authors

Fu H,Yu L,Cui M,Zhang J,Zhang X,Li Z,Wang X,Jia J,Yang Y,Yu P,Jia H,Liu B

doi

10.1016/j.bmc.2013.04.028

subject

Has Abstract

pub_date

2013-07-01 00:00:00

pages

3708-14

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(13)00354-4

journal_volume

21

pub_type

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