Gabaculine is a naturally occurring, conformationally constrained analog of GABA and an irreversible inhibitor of GABA transaminase (GABA-T; Ki = 2.9 μM).
CAS：59556-17-1
分子式：C7H9NO2.HCl
分子量：175.6
纯度：98%
存储：Store at -20°C

Background:

Gabaculine is a naturally occurring, conformationally constrained analog of GABA and an irreversible inhibitor of GABA transaminase (GABA-T; Ki = 2.9 μM). 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. 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. 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. 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.