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; d-Bicuculline methochloride)

Cat. No.: HY-137790 Purity: 99.35%
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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.

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Bicuculline methochloride Chemical Structure

Bicuculline methochloride Chemical Structure

CAS No. : 38641-83-7

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Based on 21 publication(s) in Google Scholar

Other Forms of Bicuculline methochloride:

Bicuculline methochloride Related Antibodies

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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

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 Mmodeling 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.
Correlated Product(s): /
Opposite Product(s): /

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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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 methochlorided-Bicuculline methochlorideGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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