| Title : Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors - Bodnar_2005_J.Med.Chem_48_905 |
| Author(s) : Bodnar AL , Cortes-Burgos LA , Cook KK , Dinh DM , Groppi VE , Hajos M , Higdon NR , Hoffmann WE , Hurst RS , Myers JK , Rogers BN , Wall TM , Wolfe ML , Wong E |
| Ref : Journal of Medicinal Chemistry , 48 :905 , 2005 |
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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. |
| PubMedSearch : Bodnar_2005_J.Med.Chem_48_905 |
| PubMedID: 15715459 |
Bodnar AL, Cortes-Burgos LA, Cook KK, Dinh DM, Groppi VE, Hajos M, Higdon NR, Hoffmann WE, Hurst RS, Myers JK, Rogers BN, Wall TM, Wolfe ML, Wong E (2005)
Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors
Journal of Medicinal Chemistry
48 :905
Bodnar AL, Cortes-Burgos LA, Cook KK, Dinh DM, Groppi VE, Hajos M, Higdon NR, Hoffmann WE, Hurst RS, Myers JK, Rogers BN, Wall TM, Wolfe ML, Wong E (2005)
Journal of Medicinal Chemistry
48 :905