1194687-49-4Relevant articles and documents
Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as Potent α4β2 nicotinic acetylcholine receptor ligands
Scanio, Marc J. C.,Shi, Lei,Bunnelle, William H.,Anderson, David J.,Helfrich, Rosalind J.,Malysz, John,Thorin-Hagene, Kirsten K.,Van Handel, Ceclia E.,Marsh, Kennan C.,Lee, Chih-Hung,Gopalakrishnan, Murali
, p. 7678 - 7692 (2012/01/06)
A series of diazabicyclo[3.3.0]octane substituted pyridines and pyrazines was synthesized and characterized at the α4β2 neuronal nicotinic acetylcholine receptor (nAChR). The compounds were designed to mimic the profile of ABT-089, high affinity binding ligand for the α4β2 nAChR, with limited agonist activity. Carboxamide derivatives of 3-(diazabicyclo[3.3.0] octane)-substituted pyridines or 2-(diazabicyclo[3.3.0]octane)-substituted pyrazines were found to have the desired binding and activity profile. The structure-activity relationship of these compounds is presented.
