bicuculline methiodide

**Bicuculline methiodide** is a synthetic, water-soluble quaternary salt of bicuculline, acting as a competitive antagonist at gamma-aminobutyric acid type A (**GABAA**) receptors and is widely used as a pharmacological tool in neuroscience research. By blocking GABAA receptor-mediated chloride currents, it reduces inhibitory synaptic transmission in the central nervous system, which can induce convulsions and is used experimentally to mimic epilepsy and study glutamatergic (excitatory amino acid) transmission. Bicuculline methiodide is more stable and soluble than bicuculline at physiological pH but does not readily cross the blood-brain barrier when administered systemically. It has also been reported to affect other neurotransmitter systems, such as the cholinergic system, and to block calcium-activated potassium channels. Its biological activity is generally restricted to research use, especially for dissecting GABAergic signaling and seizure mechanisms[3][4][5][8][13][15].

Other names

(-)-bicuculline methiodide1(S),9(R)-(-)-bicuculline methiodide(S)-6,6-dimethyl-5-((R)-8-oxo-6,8-dihydro-[1,3]dioxolo[4,5-e]isobenzofuran-6-yl)-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-6-ium iodide(-)-bicuculline methiodid40709-69-1CB3404287CB-3404287CB 3404287