Α3IA explained

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.[1]

This compound also has affinity for the other subunits of the GABAA receptor, but it is more selective for the α3 subunit.[2]

See also

Notes and References

  1. 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 . 10.1038/sj.bjp.0706056 . 0007-1188 . 1576012 . 15655523.
  2. 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 . 10.2147/NDT.S164307 . free . 1176-6328 . 5973310 . 29872302.

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