α3IA
Names | |
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IUPAC name Methyl 5-(4-methoxyphenyl)-1-methyl-2-oxo-6-pyridin-4-ylpyridine-3-carboxylate | |
Identifiers | |
3D model (JSmol) | |
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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). |
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
[edit]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
[edit]- α5IA, an inverse agonist at the α5 subunit of GABAA receptors
References
[edit]- ^ "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.