Art. -Nr.: HY-N0219

Bicuculline

Name: Bicuculline
Brand: MedChemExpress
SKU: HY-N0219
Price: 77.00 USD
Availability: InStock
Rating: 5 (42 reviews)

(Synonyms: (+)-Bicuculline)

42 Cited Publications

Kundenbewertung

Based on 42 publication(s) in Google Scholar

Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABA_A 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.

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Reinheit : 99.98%
CAS. Nr.: 485-49-4
Formel: C₂₀H₁₇NO₆
Molecular Weight:367.35

Speicherung:

4°C, protect from light

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

Bicuculline Chemical Structure

CAS. Nr.: 485-49-4

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Use of MCE Products

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Induced Disease Models
Chemical Information
Publications (42)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 2 μM (GABA_A)^[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 α₁β₂γ_2L GABA_A receptors^[3].

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 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 C_max 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 Modeling 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.

Chemical Information

CAS. Nr. 485-49-4
Appearance Solid
Molecular Weight 367.35
Formel C₂₀H₁₇NO₆
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
Synonyms

(+)-Bicuculline
Structure Classification
- Alkaloids
- Isoquinoline Alkaloids
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Publications (42)

All In Vivo Efficacy StudyWBIF

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Journal Impact Factor

Cell

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

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

Bicuculline 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 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 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)

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

2025 Oct 20:e07908. PMID: 41111460

Bicuculline 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)

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)

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]

2025 Feb;12(5):e2407387. PMID: 39679872

Bicuculline purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb;12(5):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
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]

2025 Jan 15:361:123290. 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
Naunyn Schmiedebergs Arch Pharmacol

2026 Jul 7. PMID: 42410225
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

2023 Jul 6.
Research Square Print

September 19th, 2022.
Research Square Print

August 24th, 2022.

Lösungsmittel & Löslichkeit

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)

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

2.7222 mL

13.6110 mL

27.2220 mL

5 mM

0.5444 mL

2.7222 mL

5.4444 mL

10 mM

0.2722 mL

1.3611 mL

2.7222 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (6.81 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (624 KB)
- English - EN (624 KB)
- Français - FR (624 KB)
- Deutsch - DE (624 KB)
- Norwegian - NO (624 KB)
- Español - ES (624 KB)
- Swedish - SV (624 KB)
- Italian - IT (624 KB)
- Korean - KR (624 KB)
- Portuguese - PT (624 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Johnston GA. Advantages of an antagonist: bicuculline and other GABA antagonists. Br J Pharmacol. 2013;169(2):328-336. [Content Brief]

[2]. Khawaled R, et al. Bicuculline block of small-conductance calcium-activated potassium channels. Pflugers Arch. 1999;438(3):314-321. [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]. Baram TZ, et al. Bicuculline induced seizures in infant rats: ontogeny of behavioral and electrocortical phenomena. Brain Res Dev Brain Res. 1990 Dec 15;57(2):291-5. [Content Brief]

[5]. P Gass, et al. Induction of immediate early gene encoded proteins in the rat hippocampus after bicuculline-induced seizures: differential expression of KROX-24, FOS and JUN proteins. Neuroscience. 1992;48(2):315-24. [Content Brief]

[6]. Jianshe Ma, et al. Determination of bicuculline in rat plasma by liquid chromatography mass spectrometry and its application in a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Mar 15:953-954:143-6. [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
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

Bioz

Keywords

Bicuculline

42 Cited Publications

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Bicuculline

Publications Citing Use of MedChemExpress (MCE) Bicuculline