Correlation Engine 2.0
Clear Search sequence regions

Sizes of these terms reflect their relevance to your search.

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.


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

Expand section icon Mesh Tags

Expand section icon Substances

PMID: 22749278

View Full Text