Radioiodinated 9-fluorenone derivatives for imaging ?7-nicotinic acetylcholine receptors.
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ABSTRACT:
SUBMITTER: Gao H
PROVIDER: S-EPMC7451070 | biostudies-literature | 2019 Dec
REPOSITORIES: biostudies-literature
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Radioiodinated 9-fluorenone derivatives for imaging α7-nicotinic acetylcholine receptors.
Gao Hang H Wang Shuxia S Qiang Bingchao B Wang Sixuan S Zhang Huabei H
MedChemComm 20191119 12
A series of 9<i>H</i>-fluoren-9-one substituents were synthesized and evaluated for imaging cerebral α7-nAChRs. <i>Meta</i>-iodine substituted 9-fluorenone <b>5</b> with high binding affinity (<i>K</i> <sub>i</sub> = 9.3 nM) and selectivity was radiolabeled with <sup>125</sup>I. Fully <i>in vitro</i> and <i>in vivo</i> studies of [<sup>125</sup>I]<b>5</b> have been performed. [<sup>125</sup>I]<b>5</b> exhibited well brain uptake with a peak concentration of 7.5 ± 0.9% ID/g in mice brains. Moreov ...[more]
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