1194687-48-3Relevant 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.
Selective Ligands for the Neuronal Nicotinic Receptors and Uses Thereof
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Page/Page column 13, (2009/12/04)
The present application describes selective ligands of formula (I) for neuronal nicotinic receptors (NNRs), more specifically for the α4β2 NNR subtype, compositions thereof, and methods of using the same, wherein X, R1, X, R2, R3, L1, m, n, p, and q are defined in the specification.