SCH-202676: An allosteric modulator of both agonist and antagonist binding to G protein-coupled receptors
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SCH-202676 is a global GPCR inhibitor that blocks agonist and antagonist binding to structurally diverse GPCRs coupling to Gαi/o, Gαs, and Gαq proteins.
“SCH-202676, a global GPCR inhibitor that blocks both agonist and antagonist binding to structurally diverse GPCRs that couple to Gαi/o, Gαs and Gαq proteins (Fawzi et al., 2001; Lewandowicz et al., 2006).”
From A Cardiovascular Disease-Linked Gut Microbial Metabolite Acts via Adrenergic Receptors (2020) · cites this paper as Fawzi et al., 2001
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Facile Synthesis of 2-Aryl-3-phenyl-5-phenylamino-2,5-dihydro-1,2,4-thiadiazole-5-carbonitriles
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- Authors
- Fawzi, A. B., Macdonald, D., Benbow, L. L., Smith-Torhan, A., Zhang, H., Weig, B. C., Ho, G., Tulshian, D., Linder, M. E., & Graziano, M. P.
- Affiliations
- Washington University in St. Louis (US)
- Corresponding author
- Fawzi, Ahmad B.
- Venue
- Molecular Pharmacology
- Publisher
- Elsevier BV
- Published
- 2001-01
- Volume
- 59
- Issue
- 1
- Pages
- 30-37
- ISSN
- 0026-895X (ISSN-L)
- OpenAlex
- W1875675415
- Cited by
- 82
- References
- 42
- Citations by year
- 2026: 1 · 2024: 4 · 2023: 7 · 2022: 3 · 2021: 1 · 2020: 6 · 2019: 2 · 2018: 1 · 2017: 2 · 2016: 2 · 2015: 2 · 2013: 1 · 2012: 3
- FWCI
- 1.52
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Molecular Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institutes of Health
- National Institute of General Medical Sciences (GM 51466, R01GM051466)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
- Keywords
- thiadiazoles, allosteric modulators, G protein-coupled receptors, receptor antagonism, receptor agonism, alpha2A-adrenergic receptor, beta2-adrenergic receptor, opioid receptors, muscarinic receptors, dopamine D1 receptor, dopamine D2 receptor, adrenergic receptors, accessory proteins
- MeSH terms
- Allosteric Regulation, Escherichia coli, Humans, Radioligand Assay, Receptors, Adrenergic, Thiadiazoles, Thiazoles, Tumor Cells, Cultured, Guanosine 5'-O-(3-Thiotriphosphate), Adrenergic Agents, HT29 Cells
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