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

Bicuculline methochloride  (Synonyms: (-)-Bicuculline methochloride)

Cat. No.: HY-137790 Purity: 99.80%
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Bicuculline ((+)-Bicuculline; d-Bicuculline) methochloride is a selective GABAA receptor antagonist with an IC50 value of 3 μM. Bicuculline methochloride induces clonic tonic convulsions in mammals and can also be used to block Ca2+ activated potassium channels. Bicuculline methochloride can be used in studies of epilepsy and other related psychiatric disorders.

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

CAS No. : 38641-83-7

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10 mM * 1 mL in Water
ready for reconstitution
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Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Bicuculline methochloride:

Bicuculline methochloride Related Antibodies

Top Publications Citing Use of Products

39 Publications Citing Use of MCE Bicuculline methochloride

In Vivo Efficacy Study
WB
IF

    Bicuculline methochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 20:e07908.  [Abstract]

    GABAA receptor antagonist (Bicuculline, 5 µg/10 µL, i.t.) weakened acute morphine analgesic effect.

    Bicuculline methochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Dec 16:e2407387.  [Abstract]

    Bicuculline (100 ng; 0.5 μL; infusion pump). Paw withdrawal responses to the 0.07 g von Frey filament following mPFC injection of physiological saline or Bicuculline (Bic) within 2 hours after intraperitoneal PTX injection.

    Bicuculline methochloride purchased from MedChemExpress. Usage Cited in: Cell. 2023 Mar 30;186(7):1352-1368.e18.  [Abstract]

    The antidepressant-like effect of activation of MGA1 in the FST was attenuated by A1 infusion of Bicuculline (BIC, 20 μM; infusion pump).

    Bicuculline methochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 Mar 28;12(7):3057-3078.

    Bicuculline (3.5 mg/kg; subcutaneous injections). Western blot analyses of Gabra1, Gabra3, Gabra5, Gabrb3, Gabrg2, KCC2 and GAPDH in the lesion sites from different groups at 4 wpt.

    Bicuculline methochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 Mar 28;12(7):3057-3078.

    Bicuculline (3.5 mg/kg; subcutaneous injections). Representative IF images of transverse spinal cord sections from the Intact, +PBS, +PBS+Bic, +MSC, and +MSC+Bic groups at 4 wpt.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Bicuculline ((+)-Bicuculline; d-Bicuculline) methochloride is a selective GABAA receptor antagonist with an IC50 value of 3 μM. Bicuculline methochloride induces clonic tonic convulsions in mammals and can also be used to block Ca2+ activated potassium channels. Bicuculline methochloride can be used in studies of epilepsy and other related psychiatric disorders[1][2].

    IC50 & Target

    IC50: 3 μM (GABAA)[3]
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    7 μM
    Compound: 7
    Inhibition of Wistar rat recombinant SK3 channel expressed in HEK293 cells by whole cell patch clamp technique
    Inhibition of Wistar rat recombinant SK3 channel expressed in HEK293 cells by whole cell patch clamp technique
    		[PMID: 18998663]
    In Vitro

    Bicuculline methochloride (1 μM and 3 μM) attains the maximal response of GABA. Bicuculline methochloride 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 human α1β2γ2L GABAA receptors expressed in Xenopus oocytes[3].
    Bicuculline methochloride (1-100 μM; 2 min; applied as outside-out patches) potently blocks both Apamin (HY-P0256)-sensitive small-conductance calcium-activated potassium channels (SK2) currents and Apamin-insensitive SK1 currents in Xenopus oocytes[4].

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

    Bicuculline methochloride 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 methochloride can be used in animal modeling to create epilepsy models. Intracerebral injection of Bicuculline methochloride causes an increase in capillary blood flow in the epileptic focus (the specific region where seizures originate), with local blood flow increasing to 42.5 red blood cells per second (compared to 27.8 red blood cells per second in areas away from the epileptic focus)[5].

    Induction of epilepsy[5]
    Background
    Epileptic seizures are closely related to the imbalance between neuronal excitability and inhibition, leading to abnormal neuronal discharges. Bicuculline methochloride is a GABAA receptor (GABAA receptor) antagonist that can inhibit inhibitory neurotransmission, induce excitatory neuronal activity, and cause population bursts (indicating that a large number of neurons fire action potentials simultaneously), thereby inducing epileptic seizures[5].
    Specific Modeling Methods
    Mice: C57BL6 • male and female • 20-30 g
    Administration: 2.5 mM • Intracranial Injection (deep layers of the somatosensory cortex) • single dose
    Note
    (1) Dissolve 2.5 mM bicuculline methochloride in physiological saline.
    (2) Inject bicuculline methochloride by inserting a glass micropipette with a diameter of 20-50 μm into the deep layers of the mouse somatosensory cortex.
    (3) Surgical operation precautions:
    a. Fix an insulated metallic head frame above the planned craniotomy area, and make a craniotomy with a diameter of approximately 3 mm over the mouse somatosensory cortex, removing the dura mater to expose the brain tissue.
    b. Gently rinse the exposed area with artificial cerebrospinal fluid (composition of artificial cerebrospinal fluid: 125 mM NaCl, 3 mM KCl, 26 mM NaHCO3, 10 mM glucose, 1.1 mM NaH2PO4, 2 mM CaCl2, 1 mM MgSO4) to maintain the physiological environment of the brain tissue.
    c. Cover the craniotomy with a phosphate-buffered saline solution containing 1% agarose (pH 7.4) and place a glass coverslip on the metal frame to protect the exposed brain tissue.
    Modeling Indicators
    Electrophysiological changes: A large number of neurons in the deep layers of the mouse somatosensory cortex fire electrical signals simultaneously, producing electrical signals characterized by interictal spikes (Note: Interictal Spikes (IISs) refer to the brief, high-amplitude voltage deflections observed in the electroencephalogram (EEG), which are typically associated with epileptic seizures).
    Blood flow changes: In the somatosensory cortex of mice injected with bicuculline methochloride, capillary blood flow significantly increases.

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

    417.84

    Formula

    C21H20ClNO6
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    C[N+]([C@](C1=C2C=C3C(OCO3)=C1)([H])[C@@](O4)([H])C(C=CC5=C6OCO5)=C6C4=O)(CC2)C.[Cl-]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    H2O : 50 mg/mL (119.66 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3933 mL 11.9663 mL 23.9326 mL
    5 mM 0.4787 mL 2.3933 mL 4.7865 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    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). 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
    H2O 1 mM 2.3933 mL 11.9663 mL 23.9326 mL 59.8315 mL
    5 mM 0.4787 mL 2.3933 mL 4.7865 mL 11.9663 mL
    10 mM 0.2393 mL 1.1966 mL 2.3933 mL 5.9832 mL
    15 mM 0.1596 mL 0.7978 mL 1.5955 mL 3.9888 mL
    20 mM 0.1197 mL 0.5983 mL 1.1966 mL 2.9916 mL
    25 mM 0.0957 mL 0.4787 mL 0.9573 mL 2.3933 mL
    30 mM 0.0798 mL 0.3989 mL 0.7978 mL 1.9944 mL
    40 mM 0.0598 mL 0.2992 mL 0.5983 mL 1.4958 mL
    50 mM 0.0479 mL 0.2393 mL 0.4787 mL 1.1966 mL
    60 mM 0.0399 mL 0.1994 mL 0.3989 mL 0.9972 mL
    80 mM 0.0299 mL 0.1496 mL 0.2992 mL 0.7479 mL
    100 mM 0.0239 mL 0.1197 mL 0.2393 mL 0.5983 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Bicuculline methochloride Related Classifications

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    • 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 methochloride38641-83-7(-)-Bicuculline methochlorideGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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