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

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 (K _i = 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 serie

SUBMITTER: Gao H 

PROVIDER: S-EPMC7451070 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature