Α3IA

α3IA[1]
Names
IUPAC name
Methyl 5-(4-methoxyphenyl)-1-methyl-2-oxo-6-pyridin-4-ylpyridine-3-carboxylate
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
  • InChI=1S/C20H18N2O4/c1-22-18(14-8-10-21-11-9-14)16(12-17(19(22)23)20(24)26-3)13-4-6-15(25-2)7-5-13/h4-12H,1-3H3
    Key: LENMNEQXCQXJHV-UHFFFAOYSA-N
  • CN1C(=C(C=C(C1=O)C(=O)OC)C2=CC=C(C=C2)OC)C3=CC=NC=C3
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

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

References

  1. ^ "Alpha3IA".
  2. ^ 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.
  3. ^ 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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