(+)-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.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 97 In stock
USD 297 In stock

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1 Customer Review

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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 (57.16 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 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 Information

Molecular Weight 367.35
Formula

C20H17NO6

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

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GABA Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID