Agastache

γ-Acetylenic GABA, also known as 4-aminohex-5-ynoic acid is a potent and irreversible inhibitor of GABA-T.^[3]

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.^[4]

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.^[5]

References

^ https://pubchem.ncbi.nlm.nih.gov/compound/4-Aminohex-5-ynoic-acid
^ "4-Aminohex-5-ynoic acid". pubchem.ncbi.nlm.nih.gov.
^ 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. 31 (2): 207. doi:10.1212/WNL.31.2.207. ISSN 0028-3878.
^ Myslobodsky, M. S.; Valenstein, E. S. (April 1980). "Amygdaloid kindling and the GABA system". Epilepsia. 21 (2): 163–175. doi:10.1111/j.1528-1157.1980.tb04058.x. hdl:2027.42/66112. ISSN 0013-9580. PMID 7358042.
^ 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. doi:10.1001/archpsyc.1980.01780250062007. ISSN 0003-990X.

[1] ttps://pubchem.ncbi.nlm.nih.gov/compound/4-Aminohex-5-ynoic-acid

[2] "4-Aminohex-5-ynoic acid". pubchem.ncbi.nlm.nih.gov.

[3] 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. 31 (2): 207. doi:10.1212/WNL.31.2.207. ISSN 0028-3878.

[4] Myslobodsky, M. S.; Valenstein, E. S. (April 1980). "Amygdaloid kindling and the GABA system". Epilepsia. 21 (2): 163–175. doi:10.1111/j.1528-1157.1980.tb04058.x. hdl:2027.42/66112. ISSN 0013-9580. PMID 7358042.

[5] 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. doi:10.1001/archpsyc.1980.01780250062007. ISSN 0003-990X.

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