2. Induced Disease Models Products Membrane Transporter/Ion Channel Neuronal Signaling
  3. Nervous System Disease Models GABA Receptor
  4. Epilepsy Models
  5. Bicuculline

Bicuculline  (Synonyms: (+)-Bicuculline; d-Bicuculline)

Cat. No.: HY-N0219 Purity: 99.97%
COA Handling Instructions

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Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice.

For research use only. We do not sell to patients.

Bicuculline Chemical Structure

Bicuculline Chemical Structure

CAS No. : 485-49-4

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10 mM * 1 mL in DMSO
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Based on 21 publication(s) in Google Scholar

Other Forms of Bicuculline:

Bicuculline Related Antibodies

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Description

Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice[1][2][3][4].

IC50 & Target

IC50: 2 μM (GABAA)[3]
In Vitro

Bicuculline (1 and 3 μM) attains the maximal response of GABA. Bicuculline appears to shift the dose–response curves of GABA in parallel to the right without decreasing GABA maximal response, suggesting that it is a competitive antagonist at α1β2γ2L GABAA receptors[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Bicuculline Related Antibodies
In Vivo

Bicuculline can be used to induce seizure models. In Sprague-Dawley rats, the pharmacokinetic parameters of orally administered Bicuculline (15 mg/kg) include a half-life of 1.6 hours, an AUC(0?t) of 109.0 ng/mL·h, a Cmax of 40 ng/mL, and a clearance rate of 144.5 L/h/kg[6].

Induction of seizures
Background
Systemic administration of Bicuculline induces generalized seizures by blockade of GABAmediated pre- and postsynaptic inhibition.
Specific Mmodeling Methods
Rat: BD IX rats • female • 140-170 g
Administration: 1.2 mg/kg • i.v. • single dose
Note
(1) Generalized seizures were induced by rapid i.v. injection of the GABAA antagonist, Bicuculline, by a dose of 1.2 mg/kg and terminated after 15 min of continuous seizures by injection of 2.5 mg/kg Diazepam.
Modeling Indicators
Molecular changes: KROX-24 and c-FOS showed a concurrent rapid rise with peak levels at 2 h and a return to Baseline levels within 8 h after seizure termination. FOS B, c-JUN and JUN B levels increased more gradually with peak intensities in the dentate gyrus reached at 4 h.
Correlated Product(s): Kainic acid (HY-N2309)
Opposite Product(s): Picrotoxin (HY-101391);Propofol (HY-B0649)

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

367.35

Formula

C20H17NO6
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C1O[C@@H]([C@H]2N(C)CCC3=C2C=C(OCO4)C4=C3)C5=CC=C(OCO6)C6=C51
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (136.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7222 mL 13.6110 mL 27.2220 mL
5 mM 0.5444 mL 2.7222 mL 5.4444 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.97%

COA (262 KB) HNMR (198 KB) LCMS (338 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7222 mL 13.6110 mL 27.2220 mL 68.0550 mL
5 mM 0.5444 mL 2.7222 mL 5.4444 mL 13.6110 mL
10 mM 0.2722 mL 1.3611 mL 2.7222 mL 6.8055 mL
15 mM 0.1815 mL 0.9074 mL 1.8148 mL 4.5370 mL
20 mM 0.1361 mL 0.6805 mL 1.3611 mL 3.4027 mL
25 mM 0.1089 mL 0.5444 mL 1.0889 mL 2.7222 mL
30 mM 0.0907 mL 0.4537 mL 0.9074 mL 2.2685 mL
40 mM 0.0681 mL 0.3403 mL 0.6805 mL 1.7014 mL
50 mM 0.0544 mL 0.2722 mL 0.5444 mL 1.3611 mL
60 mM 0.0454 mL 0.2268 mL 0.4537 mL 1.1342 mL
80 mM 0.0340 mL 0.1701 mL 0.3403 mL 0.8507 mL
100 mM 0.0272 mL 0.1361 mL 0.2722 mL 0.6805 mL
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Bicuculline Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bicuculline485-49-4(+)-Bicuculline d-BicucullineGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorconvulsantalkaloidcompetitiveneurotransmitterpotassiumSKAHPInhibitorinhibitorinhibit

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