Drug intelligence / Profile preview

picrotoxin

Development stage
Unknown
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Picrotoxin is a naturally occurring plant-derived toxin, primarily obtained from the seeds of *Anamirta cocculus*. It is a mixture of two compounds, picrotoxinin and picrotin. Picrotoxin acts as a noncompetitive antagonist at GABA A receptors (gamma aminobutyric acid type A), blocking the GABA-gated chloride ion channel. This action inhibits the main inhibitory neurotransmitter in the central nervous system, resulting in CNS stimulation and convulsant effects. Historically, it has been used as a central nervous system stimulant and as an antidote for poisoning by CNS depressants such as barbiturates. Due to its high toxicity and risk of inducing seizures or respiratory paralysis at higher doses, its clinical use is now rare; it is mainly used in research settings to study inhibitory neurotransmission[1][2][3][4][8].

Other names
cocculinFish BerryIndian BerryOriental BerryCoques de Levant
02

Targets

GABRR (GABA-A receptor subunit rho)

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