The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A Potent and Highly Selective Metabotropic Glutamate Subtype 5 Receptor Antagonist with Anxiolytic Activity
Open accessAbstract
2-Methyl-6-(phenylethynyl)pyridine (3), a potent noncompetitive mGlu5 receptor antagonist widely used to characterize the pharmacology of mGlu5 receptors, suffers from a number of shortcomings as a therapeutic agent, including off-target activity and poor aqueous solubility. Seeking to improve the properties of 3 led to the synthesis of compound 9, a highly selective mGlu5 receptor antagonist that is 5-fold more potent than 3 in the rat fear-potentiated startle model of anxiety.
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Citations
Cites
Gasparini, F., Lingenhöhl, K., Stoehr, N., Flor, P. J., Heinrich, M., Vranesic, I., Biollaz, M., Allgeier, H., Heckendorn, R., Urwyler, S., et al. (1999) · Neuropharmacology · doi:10.1016/s0028-3908(99)00082-9 · Cited by 725
Self-citation
Cited by
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders
Jeffrey Conn, P., Christopoulos, A., & Lindsley, C. W. (2009) · Nature Reviews Drug Discovery · doi:10.1038/nrd2760 · Cited by 1,063
Ionotropic and metabotropic glutamate receptor structure and pharmacology
Kew, J. N. C., & Kemp, J. A. (2005) · Psychopharmacology · doi:10.1007/s00213-005-2200-z · Cited by 788
Javitt, D. C. (2007) · International Review of Neurobiology · doi:10.1016/s0074-7742(06)78003-5 · Cited by 560
Structural insights into the activation of metabotropic glutamate receptors
Koehl, A., Hu, H., Feng, D., Sun, B., Zhang, Y., Robertson, M. J., Chu, M., Kobilka, T. S., Laeremans, T., Steyaert, J., et al. (2019) · Nature · doi:10.1038/s41586-019-0881-4 · Cited by 325
Porter, R. H. P., Jaeschke, G., Spooren, W., Ballard, T. M., Büttelmann, B., Kolczewski, S., Peters, J.-U., Prinssen, E., Wichmann, J., Vieira, E., et al. (2005) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.105.089839 · Cited by 308
Metadata
- Authors
- Cosford, N. D. P., Tehrani, L., Roppe, J., Schweiger, E., Smith, N. D., Anderson, J., Bristow, L., Brodkin, J., Jiang, X., McDonald, I., Rao, S., Washburn, M., & Varney, M. A.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2002-12-12
- Volume
- 46
- Issue
- 2
- Pages
- 204-206
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2065399310
- Cited by
- 396
- References
- 1
- FWCI
- 6.40
- Type
- journal article
- Language
- en
- Open access
- green
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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.
