(+)-Bicuculline, a light-sensitive competitive GABAA and GABAA-gated chloride channel antagonist, functions in the biochemical field as a drug, CNS stimulator, convulsant and neurotransmitter. Its chemical identities are alkaloid and phthalide-isoquinoline compound. Extracted from plant alkaloid in 1932, this metabolite has been definitively located in Adlumia fungosa, Dicentra cucullaria, Fumariaceae and some species of Corydalis. (+)-Bicuculline acts primarily on ionotropic GABAA receptors but also blocks Ca2+-activated potassium channels and can act as an agrochemical.
As a poisonous neurotoxin, it affects nervous system responses associated with GABAA by binding to the receptors but not activating them, thus inhibiting the action of gamma-aminobutyric acid. This produces a powerful convulsive reaction mimicking epilepsy and has been used in lab studies of the condition. Administered with NMDA, it has induced paraplegia. Injection to the amygdala has also produced GABA-related anxiolytic effects on emotional states.
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