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Issue 50, 2016
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Radiolabeled pyridinyl analogues of dibenzylideneacetone as β-amyloid imaging probes

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Abstract

In continuation of our investigation of the dibenzylideneacetone scaffold as Aβ imaging probes, a series of derivatives containing pyridine rings with lower lipophilicity was synthesized and evaluated. Some of these probes displayed high affinities to Aβ1–42 aggregates, which ranged from 18.0 to 8.2 nM. The high and specific binding of the radiolabeled tracers was further confirmed by in vitro autoradiography on brain sections from AD patients and transgenic mouse. In biodistribution experiments, two 18F-labeled tracers [18F]17a and [18F]18 displayed high initial brain uptake (5.05 and 6.24% ID g−1, respectively, at 2 min postinjection) and fast clearance from the brain with brain2 min/brain60 min ratios of 6.08 and 8.00. These results demonstrate that the probes [18F]17a and [18F]18 with a dibenzylideneacetone structure containing pyridine rings have great strength in imaging Aβ plaques in the brain.

Graphical abstract: Radiolabeled pyridinyl analogues of dibenzylideneacetone as β-amyloid imaging probes

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Publication details

The article was received on 27 Feb 2016, accepted on 18 Apr 2016 and first published on 20 Apr 2016


Article type: Paper
DOI: 10.1039/C6RA05168E
RSC Adv., 2016,6, 44646-44654

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    Radiolabeled pyridinyl analogues of dibenzylideneacetone as β-amyloid imaging probes

    X. Cui, X. Zhang, C. Peng, J. Dai, B. Liu and M. Cui, RSC Adv., 2016, 6, 44646
    DOI: 10.1039/C6RA05168E

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