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Synonyms | d-Bicuculline | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H17NO6 |
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分子量 | 367.35 | CAS No. | 485-49-4 | |
Solubility (25°C)* | 体外 | DMSO | 73 mg/mL warmed with 50ºC water bath (198.72 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | (+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels. |
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in vitro | (+)-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. [1] In addition to being a potent GABAA receptor antagonist, (+)-bicuculine also blocks Ca2+-activated potassium channels. [2] |
キナーゼアッセイ | Electrophysiogical recording | |
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Receptor activity is measured with two-electrode voltage- clamp techniques 2-8 days after injection. Recording microelectrodes are fabricated with a micropipette puller and filled with 3 M KCl solution. Oocytes are placed in a cell bath and voltage clamped at 60 mV. Cells are continuously superfused with ND96 buffer. The currents elicited in response to the application of drugs are recorded using a Geneclamp 500 amplifier, a Mac Lab 2e recorder, and Chart version 3.5.2 program on a Macintosh Quadra 605 computer. Drugs are tested for direct activation of GABA at GABAA receptors. For measurements of inhibitory action of drugs on receptor activation, drugs are added to the buffer solution containing GABA at the concentration producing 10%, 50%, 75%, 90% and 100% of the effect (GABA EC10, EC50, EC75, EC90 and EC100) at the receptors for constructing GABA inhibition dose-response curves. The same procedure, but with a fixed concentration of antagonists and increasing concentrations of GABA, is applied to construct GABA dose-response curves. A washout period of 3-5 min is allowed between each drug application to prevent receptor desensitisation. |
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, , Sci Rep, 2014, 4:7270.
Data from [Data independently produced by , , Br J Pharmacol, 2016, 173(10):1693-702.]
Data from [Data independently produced by , , Sci Rep, 2016, 6: 19266.]
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長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。