(+)-Bicuculline

Catalog No.S7071

(+)-Bicuculline Chemical Structure

Molecular Weight(MW): 367.35

(+)-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 DMSO USD 190 In stock
USD 97 In stock
USD 297 In stock
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3 Customer Reviews

  • Sci Rep, 2014, 4:7270.. (+)-Bicuculline purchased from Selleck.

    Blockade of sinomenine-induced anti-hyperalgesic effects by the GABAA receptor antagonist bicuculline. Filled symbols indicated significant difference in bicuculline-treated and sinomenine-treated group as compared with the sinomenine alone group. n =7-8 male rats per group.

    Br J Pharmacol, 2016, 173(10):1693-702.. (+)-Bicuculline purchased from Selleck.

  • Effects of pretreatment with different receptor antagonists on the anti-hyperalgesic effects of vitexin (10 mg/kg) in mice receiving incisional surgery. Data were expressed as mean ± SEM (n = 10-12 per group), assessed by two-way ANOVA with repeated measures followed by Bonferroni post hoc analysis. Filled black symbols indicated data significantly different from the corresponding vehicle group (P < 0.05).Both the opioid receptor antagonist naltrexone and the GABAA receptor antagonist bicuculline but not the 5-HT1A receptor antagonist WAY100635 completely blocked the anti-hyperalgesic effects of 10 mg/kg vitexin.

    Sci Rep, 2016, 6: 19266.. (+)-Bicuculline purchased from Selleck.

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Biological Activity

Description (+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
Targets
GABAA receptor [1]
2 μM
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]

Protocol

Solubility (25°C)

In vitro DMSO 21 mg/mL warmed (57.16 mM)
Water Insoluble
Ethanol 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 Information

Molecular Weight 367.35
Formula

C20H17NO6

CAS No. 485-49-4
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID