An irreversible inhibitor of GABA-T (Ki = 2.9 μM); irreversibly inhibits D-amino acid transaminase

Gabaculine (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
59556-17-1
Storage:
-20
UN-No:
Non-Hazardous - /

Gabaculine is a naturally occurring, conformationally constrained analog of GABA and an irreversible inhibitor of GABA transaminase (GABA-T; Ki = 2.9 μM).{36523} 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.{36520} 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.{36521} 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.{36522} 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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Description

An irreversible inhibitor of GABA-T (Ki = 2.9 μM); irreversibly inhibits D-amino acid transaminase, L-alanine transaminase, and L-aspartate transaminase (Kis = 0.1, 1, and 55 mM, respectively); irreversibly inhibits ornithine aminotransferase in vitro and in mouse brain and liver homogenates; increases latency to convulsion in the 3-mercaptopropionic acid-induced and minimal electroshock-induced seizure models (ED50s = 135 and 200 mg/kg, respectively); inhibits 3-mercaptopropionic acid-induced increases in GAD and GABA-T activity in mice (ED50s = 135 mg/kg); LD50 = 62 mg/kg; elevates concentrations of GABA in mouse brain by over 500% and reduces GABA-T activity to below detection limits (135 mg/kg, i.p.)

Formal name: 5-amino-1,3-cyclohexadiene-1-carboxylic acid, monohydrochloride

Synonyms: 

Molecular weight: 175.6

CAS: 59556-17-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Neuroscience|Seizure Disorders

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