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Discovery and Structure−Activity Relationship of Quinuclidine Benzamides as Agonists of α7 Nicotinic Acetylcholine Receptors
Open accessAbstract
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.
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Cites
Nicotinic receptors in the brain. Links between molecular biology and behavior
Picciotto, M. (2000) · Neuropsychopharmacology · doi:10.1016/s0893-133x(99)00146-3 · Cited by 354
Cited by
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Reymond, J.-L., & Awale, M. (2012) · ACS Chemical Neuroscience · doi:10.1021/cn3000422 · Cited by 326
Kimura, K., Tanida, M., Nagata, N., Inaba, Y., Watanabe, H., Nagashimada, M., Ota, T., Asahara, S.-I., Kido, Y., Matsumoto, M., et al. (2016) · Cell Reports · doi:10.1016/j.celrep.2016.02.032 · Cited by 84
The role of astrocytic α7 nicotinic acetylcholine receptors in Alzheimer disease
Fontana, I. C., Kumar, A., & Nordberg, A. (2023) · Nature Reviews Neurology · doi:10.1038/s41582-023-00792-4 · Cited by 86
Keever, K. R., Yakubenko, V. P., & Hoover, D. B. (2023) · Pharmacological Research · doi:10.1016/j.phrs.2023.106758 · Cited by 82
Metadata
- Authors
- 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.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2005-01-21
- Volume
- 48
- Issue
- 4
- Pages
- 905-908
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1974306203
- Cited by
- 216
- References
- 1
- FWCI
- 4.38
- Type
- journal article
- Language
- en
- Open access
- green
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- The paper
- 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. (2005). Discovery and Structure−Activity Relationship of Quinuclidine Benzamides as Agonists of α7 Nicotinic Acetylcholine Receptors. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm049363q
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
