α3IA

α3IA^[1]
Names
	IUPAC name methyl 5-(4-methoxyphenyl)-1-methyl-2-oxo-6-pyridin-4-ylpyridine-3-carboxylate
Identifiers
3D model (JSmol)	Interactive image;
ChEMBL	ChEMBL413325;
ChemSpider	9998940;
IUPHAR/BPS	4094;
PubChem CID	11824289;
	InChI 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;
	SMILES CN1C(=C(C=C(C1=O)C(=O)OC)C2=CC=C(C=C2)OC)C3=CC=NC=C3;
Properties
Chemical formula	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). Infobox references

α3IA, also known as GTPL4094 is an inverse agonist of the GABA_A 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 GABA_A receptor, but it is more selective for the α3 subunit.^[3]

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.

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[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.

[1]

[2]

[3]

Effects[edit]

See also[edit]

References[edit]