| Autor: |
Bodnar, A. L., Cortes-Burgos, L. A., Cook, K. K., Dinh, D. M., Groppi, V. E., Hajos, M., Higdon, N. R., Hoffmann, W. E., Hurst, R. S., Myers, J. K., Rogers, B. N., Wall, T. M., Wolfe, M. L., Wong, E. |
| Zdroj: |
Journal of Medicinal Chemistry; February 2005, Vol. 48 Issue: 4 p905-908, 4p |
| Abstrakt: |
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. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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