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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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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|Description||(+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.|
(+)-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. 
|In vitro||DMSO||21 mg/mL warmed (57.16 mM)|
|Water||slightly soluble or insoluble|
|Ethanol||slightly soluble or insoluble|
* 1 mg/ml means slightly soluble or insoluble.
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