α3IA
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Names | |
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IUPAC name
methyl 5-(4-methoxyphenyl)-1-methyl-2-oxo-6-pyridin-4-ylpyridine-3-carboxylate
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Identifiers | |
3D model (JSmol)
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ChEMBL | |
ChemSpider | |
PubChem CID
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Properties | |
C20H18N2O4 | |
Molar mass | 350.374 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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α3IA, also known as GTPL4094 is an inverse agonist of the GABAA receptor. It is more selective for the α3 subunit, hence its name.
Effects
Agonism of the α3 subunit shows anxiolytic properties. However, by being an inverse agonist, α3IA has the opposite action: it shows anxiogenic properties.[2]
This compound also has affinity for the other subunits of the GABAA receptor, but it is more selective for the α3 subunit.[3]
See also
- α5IA, an inverse agonist at the α5 subunit of GABAA receptors
References
- ^ "Alpha3IA".
- ^ Atack, John R.; Hutson, Peter H.; Collinson, Neil; Marshall, George; Bentley, Graham; Moyes, Christopher; Cook, Susan M.; Collins, Ian; Wafford, Keith; McKernan, Ruth M.; Dawson, Gerard R. (February 2005). "Anxiogenic properties of an inverse agonist selective for alpha3 subunit-containing GABA A receptors". British Journal of Pharmacology. 144 (3): 357–366. doi:10.1038/sj.bjp.0706056. ISSN 0007-1188. PMC 1576012. PMID 15655523.
- ^ Cheng, Tianze; Wallace, Dominique Marie; Ponteri, Benjamin; Tuli, Mahir (2018-05-23). "Valium without dependence? Individual GABAA receptor subtype contribution toward benzodiazepine addiction, tolerance, and therapeutic effects". Neuropsychiatric Disease and Treatment. 14: 1351–1361. doi:10.2147/NDT.S164307. ISSN 1176-6328. PMC 5973310. PMID 29872302.
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- GABAA receptor negative allosteric modulators
- GABAA receptor modulators
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- Pyridines
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