Bicuculline
Based on 41 publication(s) in Google Scholar
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA 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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.98%
- CAS No.: 485-49-4
- 화학식: C20H17NO6
- 분자량:367.35
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보관:
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Bicuculline
More- Cell. 2023 Mar 30;186(7):1352-1368.e18. [Abstract]
- Nat Electron. 2026 Apr 23.
- Cell Metab. 2025 Sep 23:S1550-4131(25)00383-3. [Abstract]
- Immunity. 2024 Mar 12;57(3):495-512.e11. [Abstract]
- J Adv Res. 2024 Jun:60:41-56. [Abstract]
- Theranostics. 2022 Mar 28;12(7):3057-3078. [Abstract]
- Adv Sci (Weinh). 2025 Oct 5:e11194. [Abstract]
- Adv Sci (Weinh). 2025 Oct 20:e07908. [Abstract]
- Adv Sci (Weinh). 2025 Jun 30:e03017. [Abstract]
- Adv Sci (Weinh). 2025 Feb;12(5):e2407387. [Abstract]
- J Neuroinflammation. 2026 Jan 16. [Abstract]
- Acta Pharmacol Sin. 2024 Oct;45(10):2045-2060. [Abstract]
- Proc Natl Acad Sci U S A. 2026 Mar 10;123(10):e2518983123. [Abstract]
- NPJ Parkinsons Dis. 2026 Jun 6. [Abstract]
- Neural Regen Res. 2022 Jan;17(1):178-184. [Abstract]
- Cell Rep. 2026 Jun 18;45(7):117570. [Abstract]
- Cell Rep. 2023 Nov 17;42(12):113467. [Abstract]
- Cell Rep. 2021 Jul 20;36(3):109398. [Abstract]
- Br J Pharmacol. 2026 Aug;183(15):4430-4447. [Abstract]
- Transl Psychiatry. 2026 Mar 27;16(1):210. [Abstract]
- Brain Behav Immun. 2023 Aug:112:96-117. [Abstract]
- Neurosci Bull. 2025 Jun 21. [Abstract]
- Clin Exp Hypertens. 2022 Feb 17;44(2):134-145. [Abstract]
- J Agric Food Chem. 2024 Mar 27;72(12):6189-6202. [Abstract]
- Ecotoxicol Environ Saf. 2026 Mar 15:313:119988. [Abstract]
- Life Sci. 2025 Jan 15:361:123290. [Abstract]
- Drug Des Devel Ther. 2026 Mar 10:20:566272. [Abstract]
- Neurobiol Dis. 2023 Jun 15:182:106155. [Abstract]
- Int J Mol Sci. 2022 Sep 23;23(19):11210. [Abstract]
- J Neuroendocrinol. 2020 Jun;32(6):e12876. [Abstract]
- Sci Rep. 2024 Dec 28;14(1):31388. [Abstract]
- iScience. 2025 Jun 18;28(7):112923. [Abstract]
- Biomedicines. 2021 Aug 31;9(9):1118. [Abstract]
- J Pain. 2019 May;20(5):577-591. [Abstract]
- J Psychiatr Res. 2023 Jul:163:180-194. [Abstract]
- BMC Immunol. 2022 Nov 25;23(1):58. [Abstract]
- 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.
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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WB
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IF
Biological Activity
IC50: 2 μM (GABAA)[3]
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 α1β2γ2L GABAA receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 Cmax of 40 ng/mL, and a clearance rate of 144.5 L/h/kg[6].
Administration: 1.2 mg/kg • i.v. • single dose
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 485-49-4
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Appearance Solid
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분자량 367.35
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화학식 C20H17NO6
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Color Off-white to yellow
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SMILES
O=C1O[C@@H]([C@H]2N(C)CCC3=C2C=C(OCO4)C4=C3)C5=CC=C(OCO6)C6=C51
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Synonyms
(+)-Bicuculline
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
Publications (41)
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Journal Impact Factor
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Most Recent
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Cell
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).
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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.
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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 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.
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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.
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J Neuroinflammation
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
2022 Jan;17(1):178-184. PMID: 34100454 -
Cell Rep
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
2026 Aug;183(15):4430-4447. PMID: 42062775 -
Transl Psychiatry
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
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 -
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용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (290 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
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, 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.
| 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 |
Bicuculline Related Classifications
HY-N0219 Related Classifications
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