755709-80-9Relevant academic research and scientific papers
Discovery and structure-activity relationship of quinuclidine benzamides as agonists of α7 nicotinic acetylcholine receptors
Bodnar, Alice L.,Cortes-Burgos, Luz A.,Cook, Karen K.,Dinh, Dac M.,Groppi, Vincent E.,Hajos, Mihaly,Higdon, Nicole R.,Hoffmann, William E.,Hurst, Raymond S.,Myers, Jason K.,Rogers, Bruce N.,Wall, Theron M.,Wolfe, Mark L.,Wong, Erik
, p. 905 - 908 (2005)
A library of benzamides was tested for α7 nicotinic acetylcholine receptor (nAChR) agonist activity using a chimeric receptor in a functional, cell-based, high-throughput assay. From this library, quinuclidine benzamides were found to have α7 nAChR agonist activity. The SAR diverged from the activity of this compound class verses the 5-HT3 receptor, a structural homologue of the α7 nAChR. PNU-282987, the most potent compound from this series, was also shown to open native α7 nAChRs in cultured rat neurons and to reverse an amphetamine-induced gating deficit in rats.
