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Diazaspirocyclic ligands have been synthesized in four steps as selective α4β2 nicotinic acetylcholine receptor antagonists. Structural assignment of 1-(pyridin-3-yl)-2-spiropyrrolidino-3,2'-1-azabiclo[2.2.1]heptane 2, was confirmed using a combination of NMR experiments on a key intermediate, spirolactam 9. All three target compounds synthesized in this diazaspirocyclic series exhibited high affinity (K(i)<35 nM) at the human α4β2 nAChR subtype, and very low affinity for the human α7, α3β4 (ganglion) and α1β1γδ (muscle) subtypes (K(i)>500 nM). Copyright © 2012 Elsevier Ltd. All rights reserved.

Citation

Jon-Paul Strachan, Jarrett J Farias, Jenny Zhang, William S Caldwell, Balwinder S Bhatti. Diazaspirocyclic compounds as selective ligands for the α4β2 nicotinic acetylcholine receptor. Bioorganic & medicinal chemistry letters. 2012 Aug 1;22(15):5089-92

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PMID: 22749278

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