Bicuculline methochloride  (Synonyms: (+)-Bicuculline methochloride; d-Bicuculline methochloride)

Bicuculline ((+)-Bicuculline; d-Bicuculline) methochloride is a selective GABAA receptor antagonist with an IC₅₀ value of 3 μM. Bicuculline methochloride induces clonic tonic convulsions in mammals and can also be used to block Ca²⁺ activated potassium channels. Bicuculline methochloride can be used in studies of epilepsy and other related psychiatric disorders^[1][2].

IC50: 3 μM (GABA_A)^[3]

Bicuculline 甲基氯化物 (1 μM和3 μM) 达到 GABA 的最大反应。Bicuculline 甲基氯化物似乎使 GABA的剂量-反应曲线向右平行移动，而不降低 GABA 的最大反应，这表明它在表达人 α₁β₂γ_2L GABA_A 受体的爪蟾卵母细胞中是一种竞争性拮抗剂^[3]。
Bicuculline 甲基氯化物 (1-100 μM; 2 分钟; 应用于外部贴片) 有效地阻断了爪蟾卵母细胞中，对 Apamin (HY-P0256) 敏感的小导钙活化钾通道 (SK2) 电流和对 Apamin 不敏感的 SK1 电流^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Bicuculline 甲基氯化物 (1.25-3 mg/kg; 皮下注射) 能以剂量依赖的方式引起小鼠的阵挛性抽搐，这些抽搐会因注射 μ-阿片受体激动剂吗啡而加强^[1]。
Bicuculline 甲基氯化物 (1.5-3.2 mg/kg; 皮下注射) 诱发小鼠全身性癫痫发作，对 clonus 的CD₅₀ (惊厥剂量) 为 2.2 mg/kg，对 tonus 的 CD₅₀为 2.4 mg/kg。 Bicuculline 甲基氯化物在3.2 mg/kg 的剂量下诱发的癫痫发作，可以通过 NMDA 拮抗剂 MK-801、CPP 和 CGS 19755 的预处理 (静脉注射) 来阻断^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

417.84

C₂₁H₂₀ClNO₆

38641-83-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Y Yajima, et al. Effects of differential modulation of mu-, delta- and kappa-opioid systems on bicuculline-induced convulsions in the mouse. Brain Res. 2000 Apr 17;862(1-2):120-6.  [Content Brief]

  [2]. W A Turski, et al. Excitatory amino acid antagonists protect mice against seizures induced by bicuculline. Brain Res. 1990 Apr 23;514(1):131-4.  [Content Brief]

  [3]. Huang SH, et al. Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA(A) receptors. Eur J Pharmacol. 2003;464(1):1-8.  [Content Brief]

  [4]. Khawaled R, et al. Bicuculline block of small-conductance calcium-activated potassium channels. Pflugers Arch. 1999 Aug;438(3):314-21.  [Content Brief]