Γ-Acetylenic-GABA explained

γ-Acetylenic GABA, also known as 4-aminohex-5-ynoic acid is a potent and irreversible inhibitor of GABA-T.^[1]

Mechanism of action

Like other GABA-T inhibitors, γ-acetylenic GABA causes GABA levels in the brain to be elevated. This is due to 4-aminobutyrate transaminase being the enzyme that converts γ-aminobutyric acid to L-glutamate. Inhibiting the enzyme stops this conversion from happening.

Potential uses

Anti convulsant

Continuous administration of γ-acetylenic GABA on rats during four days was able to reduce or completely stop seizures that were induced by amygdala overstimulation.^[2]

Treatment of tardive dyskinesia

A study has showed that γ-acetylenic GABA could reduce tardive dyskinesia symptoms. This result mostly happened in subjects receiving higher doses.^[3]

Notes and References

1. Tell . Guy . Böhlen . Peter . Schechter . Paul J. . Koch-Weser . Jan . Agid . Yves . Bonnet . A. M. . Coquillat . Gilles . Chazot . Guy . Fischer . Catherine . February 1981. Treatment of Huntington disease with γ ‐acetylenic GABA, an irreversible inhibitor of GABA‐ transaminase: Increased CSF GABA and homocarnosine without clinical amelioration . Neurology . en . 31 . 2 . 207 . 10.1212/WNL.31.2.207 . 0028-3878.
2. Myslobodsky . M. S. . Valenstein . E. S. . April 1980 . Amygdaloid kindling and the GABA system . Epilepsia . 21 . 2 . 163–175 . 10.1111/j.1528-1157.1980.tb04058.x . 0013-9580 . 7358042. 2027.42/66112 . free .
3. Casey . Daniel E. . Gerlach . Jes . Magelund . Gerhard . Christensen . Torben Rosted . 1980-12-01 . γ-Acetylenic GABA in Tardive Dyskinesia . Archives of General Psychiatry . 37 . 12 . 1376–1379 . 10.1001/archpsyc.1980.01780250062007 . 0003-990X.