2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Bicuculline methiodide

Bicuculline methiodide  (Synonyms: (-)-Bicuculline methiodide)

Cat. No.: HY-103474 Purity: 99.93%
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Bicuculline methiodide ((-)-Bicuculline methiodide) is a potent GABAA blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.

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

Bicuculline methiodide Chemical Structure

Bicuculline methiodide Chemical Structure

CAS No. : 40709-69-1

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

Other Forms of Bicuculline methiodide:

Bicuculline methiodide Related Antibodies

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Bicuculline methiodide

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Bicuculline methiodide ((-)-Bicuculline methiodide) is a potent GABAA blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current[1].

In Vitro

Bicuculline methiodide (30 μM) promotes N-methyl-d-aspartate (NMDA) stimulation to facilitate burst firing in dopamine neurons[1].
Cluster discharges in the lateral habenular nucleus (LHb) of the antireward center are sufficient conditions for depression to occur. LHb neurons are usually classified into three types: silent, tonic-firing, burst-firing[2].

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

Bicuculline methiodide Related Antibodies
In Vivo

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

(-)-Bicuculline methobromide (0.6 nmol/rat) attenuates the antiallodynic effect of Neurotropin[3].
(-)-Bicuculline methobromide can be used in animal modeling to create epilepsy models and is capable of crossing the blood-brain barrier[4].

1. Induction of epilepsy[4]
Background
(-)-Bisculline methoromide can inhibit the synthesis and release of GABA, and weaken GABA's inhibition of neuronal activity in the SN reticular region (SNr), leading to epilepsy.
Specific Mmodeling Methods
Rat: Sprague-Dawley (SD) • male or female • 2 weeks old
Administration: 12.5, 25, 50 or 100 ng/0.25 μL • inject into SN or corpus striatum through bilateral catheter implantation
Note
(1) Dissolve (-)-Bicuculine methoromide in distilled water and administer at a volume of 0.25 μL.
(2) Simultaneously administer bilateral infusions at a rate of 0.25 μ L/min, and after the infusion is completed, insert the catheter in situ for an additional minute to prevent drug reflux.
(3) Due to the short-lived effect of (-) - Bicuculine methoromide in SN, rats were tested 5 minutes after completing the infusion.
Modeling Indicators
Behavioral observation: Shortened the latency period of epileptic seizures, causing stereotyped behaviors such as excessive sniffing or licking, chewing movements, head twitching, and slow or occasional circling.
Correlated Product(s): Muscimol (HY-N2313)
Opposite Product(s): /

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

509.29

Formula

C21H20INO6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[N+]1([C@](C2=C(CC1)C=C3C(OCO3)=C2)([H])[C@@]4([H])C5=C(C6=C(OCO6)C=C5)C(O4)=O)C.[I-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (294.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9635 mL 9.8176 mL 19.6352 mL
5 mM 0.3927 mL 1.9635 mL 3.9270 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.91 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 10 mg/mL (19.64 mM); Clear solution; Need ultrasonic

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9635 mL 9.8176 mL 19.6352 mL 49.0879 mL
5 mM 0.3927 mL 1.9635 mL 3.9270 mL 9.8176 mL
10 mM 0.1964 mL 0.9818 mL 1.9635 mL 4.9088 mL
15 mM 0.1309 mL 0.6545 mL 1.3090 mL 3.2725 mL
20 mM 0.0982 mL 0.4909 mL 0.9818 mL 2.4544 mL
25 mM 0.0785 mL 0.3927 mL 0.7854 mL 1.9635 mL
30 mM 0.0655 mL 0.3273 mL 0.6545 mL 1.6363 mL
40 mM 0.0491 mL 0.2454 mL 0.4909 mL 1.2272 mL
50 mM 0.0393 mL 0.1964 mL 0.3927 mL 0.9818 mL
60 mM 0.0327 mL 0.1636 mL 0.3273 mL 0.8181 mL
80 mM 0.0245 mL 0.1227 mL 0.2454 mL 0.6136 mL
100 mM 0.0196 mL 0.0982 mL 0.1964 mL 0.4909 mL
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Bicuculline methiodide 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:

Bicuculline methiodide40709-69-1(-)-Bicuculline methiodideGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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