(+)-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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(+)-Bicuculline Chemical Structure

(+)-Bicuculline Chemical Structure
Molecular Weight: 367.35

Validation & Quality Control

Cited by 1 publications:

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Product Information

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Product Description

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]
IC50 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]
In vivo
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Huang SH, et al. Eur J Pharmacol, 2003, 464(1), 1-8.

[2] Khawaled R, et al. Pflugers Arch, 1999, 438(3), 314-321.

Chemical Information

Download (+)-Bicuculline SDF
Molecular Weight (MW) 367.35
Formula

C20H17NO6

CAS No. 485-49-4
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 21 mg/mL warming (57.16 mM)
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 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)-

Tech Support

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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