Drug intelligence / Profile preview

gabaculine

Development stage
Discontinued
Modality
Small Molecules
Administration
Intravenous (in Animal Studies)
01

Overview

Gabaculine is a naturally occurring neurotoxin and experimental small molecule that acts as a potent and irreversible inhibitor of GABA transaminase (GABA-T), the enzyme responsible for metabolizing gamma-aminobutyric acid (GABA) in the brain. It is also reported to inhibit GABA reuptake. Gabaculine was first isolated from the bacterium Streptomyces toyacaensis. By inhibiting GABA-T, gabaculine increases brain GABA levels and has demonstrated anticonvulsant effects in animal models. However, its high toxicity at anticonvulsant doses has precluded its development as a therapeutic drug; it remains primarily a research tool for studying GABAergic neurotransmission and epilepsy[2][3][9].

Other names
gabaculin(S)-gabaculine
02

Targets

GAT (GABA transporter family)ABAT (4-aminobutyrate aminotransferase)

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