The DOI matches its Crossref record.
Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity of N-(4-(2-Methoxyphenoxy)phenyl)-N-(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine
Open accessAbstract
This report describes recently discovered novel allosteric modulators of metabotropic glutamate2 (mGlu2) receptors. These pyridylmethylsulfonamides (e.g., 3) potentiate glutamate, shifting agonist potency by 2-fold. This effect was specific for mGlu2 (vs mGlu1,3-8 receptors). Also, 3 failed to potentiate a chimeric mGlu2/1 receptor, demonstrating the mGlu2 transmembrane region's critical involvement. In a fear-potentiated startle model, 3 showed anxiolytic activity that was prevented by mGlu2/3 antagonist pretreatment. Thus, these pyridylmethylsulfonamides represent the first mGlu2 receptor potentiators discovered.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
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
Metabotropic glutamate receptors as novel targets for anxiety and stress disorders
Swanson, C. J., Bures, M., Johnson, M. P., Linden, A.-M., Monn, J. A., & Schoepp, D. D. (2005) · Nature Reviews Drug Discovery · doi:10.1038/nrd1630 · Cited by 607
Self-citationPotential Psychiatric Applications of Metabotropic Glutamate Receptor Agonists and Antagonists
Krystal, J. H., Mathew, S. J., DʼSouza, D. C., Garakani, A., Gunduz-Bruce, H., & Charney, D. S. (2010) · CNS Drugs · doi:10.2165/11533230-000000000-00000 · Cited by 180
Johnson, M. P., Barda, D., Britton, T. C., Emkey, R., Hornback, W. J., Jagdmann, G. E., McKinzie, D. L., Nisenbaum, E. S., Tizzano, J. P., & Schoepp, D. D. (2005) · Psychopharmacology · doi:10.1007/s00213-004-2099-9 · Cited by 156
Self-citation
Metadata
- Authors
- Johnson, M. P., Baez, M., Jagdmann, G. E., Britton, T. C., Large, T. H., Callagaro, D. O., Tizzano, J. P., Monn, J. A., & Schoepp, D. D.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2003-06-12
- Volume
- 46
- Issue
- 15
- Pages
- 3189-3192
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1990246915
- Cited by
- 182
- References
- 0
- FWCI
- 4.22
- Type
- journal article
- Language
- en
- Open access
- green
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
Data sources
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.
