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| 品牌 | absin | CAS | 485-49-4 |
|---|---|---|---|
| 分子式 | C20H17NO6 | 纯度 | ≥98% |
| 分子量 | 367.36 | 货号 | abs812832 |
| 规格 | 50mg | 供货周期 | 现货 |
| 主要用途 | is an antagonist of the GABAA receptor. | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
（+）-Bicuculline 485-49-4
| 产品描述 | |
| 描述 | (+)-Bicuculline is an antagonist of the GABAA receptor. (+)-Bicuculline is the parent compound of the water soluble N-methyl derivatives (-)-Bicuculline methiodide and (-)-Bicuculline methobromide . Antagonism of the GABAA receptor by (+)-Bicuculline blocks the neurotransmission inhibition function of the GABA system in vitro. |
| 应用 | A GABA A receptor antagonist |
| 纯度 | ≥98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 毕扣扣灵(碱)，荷包牡丹碱；山乌龟碱 |
| 外观 | 淡黄色结晶粉末 |
| 可溶性/溶解性 | DMSO ：21 mg/mL warmed (57.16 mM) |
| 生物活性 | |
| 靶点 | GABAA receptor |
| In vitro(体外研究) | (+)-Bicuculline (1-100μM) dose-dependently inhibits the Cl- conductance generated by 40 μM GABA. (+)-Bicuculline also inhibits the agonist action of GABA at 40 μM at α1β2γ2L receptors. (+)-Bicuculline at 1 and 3 μM increases GABA EC50 values 1.6 times (41.0-67.0 μM) and 3.6 times (36.1-129.0 μM), respectively. Atα1β2γ2L GABAA receptors, (+)-bicuculline displays the general property of the competitive antagonist, producing a parallel shift of GABA concentration-effect curves and having no effect on the maximal response of GABA. In addition to being a potent GABAA receptor antagonist, (+)-bicuculine also blocks Ca2+-activated potassium channels. |
| 参考文献 | |
| 参考文献 | [1] Huang SH, et al. Eur J Pharmacol, 2003, 464(1), 1-8. [2] Khawaled R, et al. Pflugers Arch, 1999, 438(3), 314-321. |
| 研究领域 | |
| 研究领域 | Neuroscience Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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