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Radioiodinated 9-fluorenone derivatives for imaging α7-nicotinic acetylcholine receptors

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Abstract

A series of 9H-fluoren-9-one substituents were synthesized and evaluated for imaging cerebral α7-nAChRs. Meta-iodine substituted 9-fluorenone 5 with high binding affinity (Ki = 9.3 nM) and selectivity was radiolabeled with 125I. Fully in vitro and in vivo studies of [125I]5 have been performed. [125I]5 exhibited well brain uptake with a peak concentration of 7.5 ± 0.9% ID/g in mice brains. Moreover, ex vivo autoradiography studies and micro single-photon emission computed tomography (micro-SPECT/CT) dynamic imaging in mice confirmed its in vivo imaging properties. Besides, molecular docking and MD studies were also performed to interpret the binding mechanisms of the two series of ligands towards α7-nAChRs. To conclude, the meta-iodine substituted 9-fluorenone [125I]5 could be a promising tracer for imaging α7-nAChRs.

Graphical abstract: Radioiodinated 9-fluorenone derivatives for imaging α7-nicotinic acetylcholine receptors

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Publication details

The article was received on 27 Aug 2019, accepted on 14 Oct 2019 and first published on 19 Nov 2019


Article type: Research Article
DOI: 10.1039/C9MD00415G
Med. Chem. Commun., 2019, Advance Article

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    Radioiodinated 9-fluorenone derivatives for imaging α7-nicotinic acetylcholine receptors

    H. Gao, S. Wang, B. Qiang, S. Wang and H. Zhang, Med. Chem. Commun., 2019, Advance Article , DOI: 10.1039/C9MD00415G

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