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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[1][2][3]. 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. | [in vivo]
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. DOI:10.1001/archpsyc.1980.01780250062007
[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. DOI:10.1016/0014-2999(78)90138-3
[3] Alabed S, et, al. Gamma-aminobutyric acid agonists for neuroleptic-induced tardive dyskinesia. Cochrane Database Syst Rev. 2011 Apr 13;(4):CD000203. DOI:10.1002/14651858.CD000203.pub3 |
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