Antibodies
(+)-Bicuculline
- 貨號 Cat. No.
- S7071
- 規格 Size
- 10mM/1mL~250mg
- 品牌 Brand
- Selleckchem
Description
(+)-Bicuculline
Catalog No.S7071
(+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | (+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels. | |||||
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| Targets | GABAA | |||||
| IC50 | 2 μM [1] | |||||
| 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. Atα1β2γ2LGABAA 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] | |||||
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| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Electrophysiogical recording | 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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References
Chemical Information
| Molecular Weight (MW) | 367.35 |
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| Formula | C20H17NO6 |
| CAS No. | 485-49-4 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | D-Bicuculline |
| Solubility (25°C) * | In vitro | DMSO | 74 mg/mL (201 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <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. | |||
| Chemical Name | Furo[3,4-e]-1,3-benzodioxol-8(6H)-one, 6-[(5S)-5,6,7,8-tetrahydro-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl]-, (6R)- |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.36735 | 3.6735 | 7.347 | 11.0205 |
