Susan M O'Connor, Brad E Sleebs, Ian P Street, Bernard L Flynn, Jonathan B Baell, Carolyn Coles, Nurul Quazi, Dharam Paul, Etienne Poiraud, Bertrand Huyard, Stephanie Wagner, Emile Andriambeloson, Errol B de Souza
This work describes the characterization of BNC210 (6-[(2,3-dihydro-1H-inden-2-yl)amino]-1-ethyl-3-(4-morpholinylcarbonyl)-1,8-naphthyridin-4(1H)-one), a selective, small molecule, negative allosteric modulator (NAM) of α7 nicotinic acetylcholine receptors (α7 nAChR). With the aim to discover a non-sedating, anxiolytic compound BNC210 was identified during phenotypic screening of a focused medicinal chemistry library using the mouse Light Dark (LD) box to evaluate anxiolytic-like activity and the mouse Open Field (OF) (dark) test to detect sedative and/or motor effects...
January 5, 2024: Neuropharmacology