αあるふぁ3IA

αあるふぁ3IA^[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

αあるふぁ3IA, also known as GTPL4094, is an inverse agonist of the GABA_A receptor. It is more selective for the αあるふぁ3 subunit, hence its name.

Effects

Agonism of the αあるふぁ3 subunit shows anxiolytic properties. However, by being an inverse agonist, αあるふぁ3IA 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 αあるふぁ3 subunit.^[3]

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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[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

See also

References