| Literature DB >> 15715459 |
Alice L Bodnar1, Luz A Cortes-Burgos, Karen K Cook, Dac M Dinh, Vincent E Groppi, Mihaly Hajos, Nicole R Higdon, William E Hoffmann, Raymond S Hurst, Jason K Myers, Bruce N Rogers, Theron M Wall, Mark L Wolfe, Erik Wong.
Abstract
A library of benzamides was tested for alpha7 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 alpha7 nAChR agonist activity. The SAR diverged from the activity of this compound class verses the 5-HT(3) receptor, a structural homologue of the alpha7 nAChR. PNU-282987, the most potent compound from this series, was also shown to open native alpha7 nAChRs in cultured rat neurons and to reverse an amphetamine-induced gating deficit in rats.Entities:
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Year: 2005 PMID： 15715459 DOI： 10.1021/jm049363q
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446