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Bicuculline methobromide

CAS No. : 66016-70-4

MCE 站：Bicuculline methobromide

产品活性：Bicuculline methobromide 是一种选择性GABAA 受体 (GABAA receptor) 拮抗剂，IC₅₀ 值为 3 μM。Bicuculline methobromide 在哺乳动物中可以诱导阵挛性强直性惊厥，还可用于阻断 Ca²⁺ 激活的钾通道。Bicuculline methobromide 可用于癫痫等相关精神疾病的研究。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：GABA Receptor

In Vitro: Bicuculline methobromide (1 μM ａnd 3 μM) attains the maximal response of GABA. Bicuculline methobromide appears to shift the doseresponse curves of GABA in parallel to the right without decreasing GABA maximal response, suggesting that it is a competitive antagonist at human α₁β₂γ_2L GABA_A receptors expressed in Xenopus oocytes.
Bicuculline methobromide (1-100 μM; 2 min; applied as outside-out patches) potently blocks both Apamin (HY-P0256)-sensitive small-conductance calcium-activated potassium channels (SK2) currents ａnd Apamin-insensitive SK1 currents in Xenopus oocytes.

In Vivo: 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.
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 CD₅₀ of 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.

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