Bicuculline methobromide is a selectiveGABAA receptorantagonist with anIC₅₀value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca²⁺activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders^[1][2].

Bicuculline methobromide (1 μM and 3 μM) attains the maximal response of GABA. Bicuculline methobromide appears to shift the dose–response curves of GABA in parallel to the right without decreasing GABA maximal response, suggesting that it is a competitive antagonist at human α₁β₂γ_2LGABA_Areceptors expressed inXenopusoocytes^[3].
Bicuculline methobromide (1-100 μM; 2 min; applied as outside-out patches) potently blocks bothApamin(HY-P0256)-sensitive small-conductance calcium-activated potassium channels (SK2) currents and Apamin-insensitive SK1 currents inXenopusoocytes^[4].

Bicuculline methobromide (subcutaneous injection, 1.25-3 mg/kg) can cause clonus-tonic convulsions in a dose-dependent manner in mice and these convulsions are enhanced by injection of the μ-opioid agonist morphine^[1].
Bicuculline methobromide (subcutaneous injection, 1.5-3.2 mg/kg) induces male Swiss S mice generalized seizures with a CD₅₀(convulsant dose) of 2.2 mg/kg for clonus and CD₅₀of 2.4 mg/kg for tonus. Seizures induced by Bicuculline at the dose of 3.2 mg/kg can be blocked by pretreatment (i.p.) with the NMDA antagonists MK-801, CPP and CGS 19755^[2].

462.29

C₂₁H₂₀BrNO₆

66016-70-4

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