γ-Acetylenic GABA (GAG) hydrochloride is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA hydrochloride can increase the concentration of GABA in rat brain. γ-Acetylenic GABA (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
γ-Acetylenic GABA hydrochloride (100 mg/kg i.p.) inhibits GABA-transaminase activity and causes a several-fold increase in the concentration of GABA in rat brain[2].
References:
[1]. Casey DE, et, al. gamma-Acetylenic GABA in tardive dyskinesia. Arch Gen Psychiatry. 1980 Dec;37(12):1376-9.
[2]. Palfreyman MG, et, al. The effect of gamma-acetylenic GABA, an enzyme-activated irreversible inhibitor of GABA-transaminase, on dopamine pathways of the extrapyramidal and limbic systems. Eur J Pharmacol. 1978 Aug 15;50(4):325-36.
[3]. Alabed S, et, al. Gamma-aminobutyric acid agonists for neuroleptic-induced tardive dyskinesia. Cochrane Database Syst Rev. 2011 Apr 13;(4):CD000203.