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Bioorg Med Chem. 2013 May 1;21(9):2635-42. doi: 10.1016/j.bmc.2013.02.018. Epub 2013 Feb 22.

Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.

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Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmacy, Research Site Leipzig, Dept. of Neuroradiopharmaceuticals, Permoserstrasse 15, 04318 Leipzig, Germany.


[(18)F]NS14490, a new potential radiotracer for neuroimaging of α7 nicotinic acetylcholine receptors (α7 nAChRs), was synthesized and evaluated in vitro and in vivo. Radioligand binding studies using [(3)H]methyllycaconitine and NS14490 as competitor showed a good target affinity (K(i,α7) = 2.5 nM) and a high selectivity towards other nAChRs. Radiosynthesis of [(18)F]NS14490 was performed by two different labelling procedures: a two-step synthesis using a prosthetic group, which led to 7% labelling yield, and the convenient direct nucleophilic substitution of the corresponding tosylate precursor, which resulted in 70% labelling yield. After optimisation of the isolation, purification and formulation process, biodistribution studies were performed in CD-1 mice. The brain uptake of [(18)F]NS14490 was comparably low (0.16% ID g(-1) wet weight at 5 min p.i.). The radiotracer showed a high metabolic stability in plasma and brain. Also, the target specificity was proven by pre-administration of a highly affine α7 ligand providing a rationale basis for further in vivo evaluation.

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