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Gabaculine is a naturally occurring, conformationally constrained analog of GABA and an irreversible inhibitor of GABA transaminase (GABA-T; Ki = 2.9 μM). [1] It irreversibly inhibits D-amino acid transaminase, L-alanine transaminase, and L-aspartate transaminase with Ki values of 0.1, 1, and 55 mM, respectively.[2] Gabaculine also irreversibly inhibits ornithine aminotransferase in vitro and in mouse brain and liver homogenates, where ornithine aminotransferase activity is suppressed for over 24 hours when administered at a dose of 50 mg/kg. [3] Gabaculine increases latency to convulsion in the 3-mercaptopropionic acid-induced and minimal electroshock-induced seizure models (ED50s = 135 and 200 mg/kg, respectively) and inhibits 3-mercaptopropionic acid-induced increases in glutamic acid decarboxylase (GAD) activity and GABA-T activity in mice (ED50s =135 mg/kg), however, the doses fall above the LD50 value of 62 mg/kg. [4] Gabaculine (135 mg/kg, i.p.) elevates concentrations of GABA in mouse brain by over 500% and knocks out GABA-T activity to below detection limits.

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