Cat. No.: HY-137790

Bicuculline methochloride

(Synonyms: (-)-Bicuculline methochloride)

43 Cited Publications

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Based on 43 publication(s) in Google Scholar

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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Pureté: 99.80%
CAS No.: 38641-83-7
Formule: C₂₁H₂₀ClNO₆
Masse moléculaire:417.84

Stockage:

4°C, sealed storage, away from moisture

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

Bicuculline methochloride Chemical Structure

CAS No.: 38641-83-7

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Induced Disease Models
Chemical Information
Publications (43)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 3 μM (GABA_A)^[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 α₁β₂γ_2L GABA_A 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.

Induced Disease Models

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 GABA_A 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.

Chemical Information

CAS No. 38641-83-7
Appearance Solid
Masse moléculaire 417.84
Formule C₂₁H₂₀ClNO₆
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-]
Synonyms

(-)-Bicuculline methochloride
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

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

Publications (43)

All In Vivo Efficacy StudyWBIF

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Cell

A thalamic-primary auditory cortex circuit mediates resilience to stress. [Abstract]

2023 Mar 30;186(7):1352-1368.e18. PMID: 37001500

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).
Nat Electron

2026 Apr 23.
Cell Metab

Hepatic acetyl-CoA metabolism modulates neuroinflammation and depression susceptibility via acetate. [Abstract]

2025 Sep 23:S1550-4131(25)00383-3. PMID: 40992374
Immunity

Disruption of the Na+/K+-ATPase-purinergic P2X7 receptor complex in microglia promotes stress-induced anxiety. [Abstract]

2024 Mar 12;57(3):495-512.e11. PMID: 38395698
J Adv Res

Gut microbial GABAergic signaling improves stress-associated innate immunity to respiratory viral infection. [Abstract]

2024 Jun:60:41-56. PMID: 37353002
Theranostics

hUC-MSC-mediated recovery of subacute spinal cord injury through enhancing the pivotal subunits β3 and γ2 of the GABAA receptor. [Abstract]

2022 Mar 28;12(7):3057-3078. PMID: 35547766

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

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. [Abstract]

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.
Adv Sci (Weinh)

Assessing the Nature of Human Brain-Derived Extracellular Vesicles on Synaptic Activity Via the Development of an Air-liquid Microfluidic Platform. [Abstract]

2025 Oct 5:e11194. PMID: 41047484
Adv Sci (Weinh)

Morphine Tolerance Gated through EZH2-Mediated Suppression of Trpc5 in Spinal GABAergic Interneurons in Male Mice. [Abstract]

2025 Oct 20:e07908. PMID: 41111460

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.
Adv Sci (Weinh)

Parvalbumin Interneuron-Dependent Hippocampal Neurogenesis Evoked by Prolonged Rhythmic Light Flicker. [Abstract]

2025 Jun 30:e03017. PMID: 40586216
Adv Sci (Weinh)

DNMT3a Downregulation Ttriggered Upregulation of GABAA Receptor in the mPFC Promotes Paclitaxel-Induced Pain and Anxiety in Male Mice. [Abstract]

2024 Dec 16:e2407387. PMID: 39679872

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.
J Neuroinflammation

Targeting the intestinal TLR4-GABAA axis to promote stroke recovery. [Abstract]

2026 Jan 16. PMID: 41546093
Acta Pharmacol Sin

Effects of Kv1.3 knockout on pyramidal neuron excitability and synaptic plasticity in piriform cortex of mice. [Abstract]

2024 Oct;45(10):2045-2060. PMID: 38862816
Proc Natl Acad Sci U S A

Neutralization of acyl-CoA-binding protein attenuates glucocorticoid-mediated suppression of cancer immunosurveillance. [Abstract]

2026 Mar 10;123(10):e2518983123. PMID: 41779791
NPJ Parkinsons Dis

Metabotropic signaling downstream of GABAA receptors suppresses neuroinflammation in Parkinson's disease. [Abstract]

2026 Jun 6. PMID: 42251036
Neural Regen Res

Polygalasaponin F protects hippocampal neurons against glutamate-induced cytotoxicity. [Abstract]

2022 Jan;17(1):178-184. PMID: 34100454
Cell Rep

A central amygdala-locus coeruleus pathway mediating pain under chronic stress. [Abstract]

2026 Jun 18;45(7):117570. PMID: 42313564
Cell Rep

Entorhinohippocampal cholecystokinin modulates spatial learning by facilitating neuroplasticity of hippocampal CA3-CA1 synapses. [Abstract]

2023 Nov 17;42(12):113467. PMID: 37979171
Cell Rep

Neuronal activity recruits the CRTC1/CREB axis to drive transcription-dependent autophagy for maintaining late-phase LTD. [Abstract]

2021 Jul 20;36(3):109398. PMID: 34289350
Br J Pharmacol

The paraventricular thalamus is required for homeostatic sleep regulation by adenosine. [Abstract]

2026 Aug;183(15):4430-4447. PMID: 42062775
Transl Psychiatry

CCK2R regulates METH-induced CPP acquisition within VTA-BLA-BNST circuit in male mice. [Abstract]

2026 Mar 27;16(1):210. PMID: 41888094
Brain Behav Immun

The microglial innate immune receptors TREM-1 and TREM-2 in the anterior cingulate cortex (ACC) drive visceral hypersensitivity and depressive-like behaviors following DSS-induced colitis. [Abstract]

2023 Aug:112:96-117. PMID: 37286175
Brain Behav Immun

Trans-cinnamaldehyde improves neuroinflammation-mediated NMDA receptor dysfunction and memory deficits through blocking NF-κB pathway in presenilin1/2 conditional double knockout mice. [Abstract]

2019 Nov:82:45-62. PMID: 31376499
Neurosci Bull

Restoration of Extrasynaptic/Synaptic GABAAR-α5 Localization Improves Sevoflurane-Induced Early Memory Impairment in Aged Mice. [Abstract]

2025 Jun 21. PMID: 40542952
Clin Exp Hypertens

Overexpression of NaV1.6 in the rostral ventrolateral medulla in rats mediates stress-induced hypertension via glutamate regulation. [Abstract]

2022 Feb 17;44(2):134-145. PMID: 34994674
J Agric Food Chem

Potential Mechanisms of Casein Hexapeptide YPVEPF on Stress-Induced Anxiety and Insomnia Mice and Its Molecular Effects and Key Active Structure. [Abstract]

2024 Mar 27;72(12):6189-6202. PMID: 38501577
Ecotoxicol Environ Saf

Cognitive behavioral dysregulation induced by low-level lead, cadmium, and mercury co-exposure is linked to AMPA receptor-associated with E/I imbalance. [Abstract]

2026 Mar 15:313:119988. PMID: 41806666
Life Sci

The modulation of cholecystokinin receptor 1 in the NAc core input from VTA on METH-induced CPP acquisition. [Abstract]

2024 Dec 3:123290. PMID: 39638282
Drug Des Devel Ther

High-Dose Propofol Induces Cytotoxicity by Elevating Intracellular Ca2⁺ via GABAA Receptor and IP3R in HT22 Cells. [Abstract]

2026 Mar 10:20:566272. PMID: 41836532
Neurobiol Dis

Contribution of activating lateral hypothalamus-lateral habenula circuit to nerve trauma-induced neuropathic pain in mice. [Abstract]

2023 Jun 15:182:106155. PMID: 37182721
Int J Mol Sci

Inhibition of GABAAR or Application of Lactobacillus casei Zhang Alleviates Ulcerative Colitis in Mice: GABAAR as a Potential Target for Intestinal Epithelial Renewal and Repair. [Abstract]

2022 Sep 23;23(19):11210. PMID: 36232509
J Neuroendocrinol

The caudal neurosecretory system: A novel thermosensitive tissue and its signal pathway in olive flounder (Paralichthys olivaceus). [Abstract]

2020 Jun;32(6):e12876. PMID: 32542811
Sci Rep

Intervention effect of regulating GABA-A receptor activity on the formation of experimental abdominal aortic aneurysm in rats. [Abstract]

2024 Dec 28;14(1):31388. PMID: 39732918
iScience

The lateral habenula contributes to regulation of body temperature. [Abstract]

2025 Jun 18;28(7):112923. PMID: 40678505
Biomedicines

Salusin-β in Intermediate Dorsal Motor Nucleus of the Vagus Regulates Sympathetic-Parasympathetic Balance and Blood Pressure. [Abstract]

2021 Aug 31;9(9):1118. PMID: 34572305
J Pain

Alleviation of Mechanical Allodynia by 14,15-Epoxyeicosatrienoic Acid in a Central Poststroke Pain Model: Possible Role of Allopregnanolone and δ-Subunit-Containing Gamma-Aminobutyric Acid A Receptors. [Abstract]

2019 May;20(5):577-591. PMID: 30500366
J Psychiatr Res

Roles of nucleus accumbens shell small-conductance calcium-activated potassium channels in the conditioned fear freezing. [Abstract]

2023 Jul:163:180-194. PMID: 37216772
BMC Immunol

Propofol maintains Th17/Treg cell balance in elderly patients undergoing lung cancer surgery through GABAA receptor. [Abstract]

2022 Nov 25;23(1):58. PMID: 36434505
bioRxiv

2025 June 03.
Research Square Preprint

2024 Oct 08.
bioRxiv

2024 November 26.
bioRxiv

2023 Jul 6.
Research Square Print

September 19th, 2022.
Research Square Print

August 24th, 2022.

Solvant et solubilité

In Vitro:

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

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3933 mL

11.9663 mL

23.9326 mL

5 mM

0.4787 mL

2.3933 mL

4.7865 mL

10 mM

0.2393 mL

1.1966 mL

2.3933 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Références

[1]. Y Yajima, et al. Effects of differential modulation of mu-, delta- and kappa-opioid systems on bicuculline-induced convulsions in the mouse. Brain Res. 2000 Apr 17;862(1-2):120-6. [Content Brief]

[2]. W A Turski, et al. Excitatory amino acid antagonists protect mice against seizures induced by bicuculline. Brain Res. 1990 Apr 23;514(1):131-4. [Content Brief]

[3]. Huang SH, et al. Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA(A) receptors. Eur J Pharmacol. 2003;464(1):1-8. [Content Brief]

[4]. Khawaled R, et al. Bicuculline block of small-conductance calcium-activated potassium channels. Pflugers Arch. 1999 Aug;438(3):314-21. [Content Brief]

[5]. Hirase H, et al. Capillary level imaging of local cerebral blood flow in bicuculline-induced epileptic foci. Neuroscience. 2004;128(1):209-16. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Bicuculline methochloride

43 Cited Publications

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Bicuculline methochloride

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

GABA Receptor Compound Library

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Publications Citing Use of MedChemExpress (MCE) Bicuculline methochloride

Activité biologique

Chemical Information

Publications (43)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Bicuculline methochloride

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

GABA Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Bicuculline methochloride

Activité biologique

Chemical Information

Publications (43)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Bicuculline methochloride Related Classifications

HY-137790 Related Classifications