Gabazine
Based on 15 publication(s) in Google Scholar
Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
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- Pureté: 98.72%
- CAS No.: 104104-50-9
- Formule: C15H18BrN3O3
- Masse moléculaire:368.23
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) Gabazine
More- Nature. 2025 Oct;646(8087):1243-1253. [Abstract]
- Cell. 2026 Jun 11;189(12):3571-3588.e27. [Abstract]
- Nat Neurosci. 2026 May 15. [Abstract]
- Nat Neurosci. 2023 May;26(5):751-764. [Abstract]
- Genes Dis. 2026 May 22.
- Phytomedicine. 2022 Jan 29;98:153965. [Abstract]
- Mol Psychiatry. 2026 Mar 23. [Abstract]
- Acta Pharmacol Sin. 2025 Sep 10. [Abstract]
- Biochem Pharmacol. 2026 Apr 19;250(Pt 1):117995. [Abstract]
- Neuropharmacology. 2026 Nov 1:298:111043. [Abstract]
- iScience. 2023 Mar 3;26(4):106322. [Abstract]
- Res Sq. 2026 Apr 21.
- Elife. 2024 May 29.
- bioRxiv. 2023 Jul 22:2023.04.28.538437. [Abstract]
- Oxid Med Cell Longev. 2022 Apr 15;2022:3716609. [Abstract]
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
Activité biologique
0.2 μM (GABA receptor)[1].
Both bicuculline and Gabazine (SR 95531) have been characterized as competitive inhibitors of GABA binding to the GABAA receptor. Gabazine is more potent than bicuculline at blocking currents elicited by GABA, with an IC50 for currents elicited by 3 μM GABA of ~0.2 μM and a Hill coefficient of 1.0. Gabazine reduces the currents elicited by 10 μM alphaxalone by ~30%, for responses of receptors containing wildtype β2 subunits. The concentration of Gabazine requires producing half the maximal block is ~0.2 μM. Gabazine also could only produce a partial block of currents gated by 300 μM pentobarbital. The maximal reduction, again, is ~30%, and the concentration of Gabazine required to produce half the maximal block is ~0.15 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 104104-50-9
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Appearance Solid
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Masse moléculaire 368.23
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Formule C15H18BrN3O3
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Color White to off-white
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SMILES
O=C(O)CCCN1C(C=CC(C2=CC=C(OC)C=C2)=N1)=N.[H]Br
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Synonyms
SR95531
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (15)
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Journal Impact Factor
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Most Recent
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Nature
2025 Oct;646(8087):1243-1253. PMID: 40931078
Gabazine purchased from MedChemExpress. Usage Cited in: Nature. 2025 Oct;646(8087):1243-1253. [Abstract]
A small fraction of the currents remained in two cells, after d-AP5 exposure, presented a shape consistent with GABAA receptor-mediated currents and could be inhibited with the GABAA receptor blocker Gabazine (Gbz) (12.5 μM).
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Cell
2026 Jun 11;189(12):3571-3588.e27. PMID: 42019490 -
Nat Neurosci
Excitatory synapses onto axonic spines jump-start action potentials and route information flow. [Abstract]2026 May 15. PMID: 42141306 -
Nat Neurosci
Emergence of consciousness from anesthesia through ubiquitin degradation of KCC2 in the ventral posteromedial nucleus of the thalamus. [Abstract]2023 May;26(5):751-764. PMID: 36973513 -
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Phytomedicine
Geraniol enhances inhibitory inputs to the paraventricular thalamic nucleus and induces sedation in mice. [Abstract]2022 Jan 29;98:153965. PMID: 35144136 -
Mol Psychiatry
BDNF restores impaired long-term potentiation of GABAergic synapses induced by chronic ethanol exposure in the VTA and attenuates reward-seeking behavior. [Abstract]2026 Mar 23. PMID: 41872517 -
Acta Pharmacol Sin
GluN2A-NMDA receptor inhibition disinhibits the prefrontal cortex, reduces forced swim immobility, and impairs sensorimotor gating. [Abstract]2025 Sep 10. PMID: 40931040 -
Biochem Pharmacol
Cipepofol attenuates endothelial barrier dysfunction in acute lung injury through DUSP1-dependent suppression of MAPK signaling. [Abstract]2026 Apr 19;250(Pt 1):117995. PMID: 42013957 -
Neuropharmacology
GPR139-mediated cholinergic circuit from the medial septum to the ventral hippocampal CA3 modulates cognitive impairment in Alzheimer's disease. [Abstract]2026 Nov 1:298:111043. PMID: 42218995 -
iScience
Synaptic scaling of corticostriatal circuits underlies hyperactivity in GABA Transporter-1 deficient mice. [Abstract]2023 Mar 3;26(4):106322. PMID: 36968092 -
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Gabazine purchased from MedChemExpress. Usage Cited in: Elife. 2024 May 29.
The effects of ICV injection of different doses of Gabazine (2 or 4 μg/mL; 2000 nL) on the recovery time of midazolam. Compared with the vehicle, ICV injection of Gabazine could reduce the recovery time.
Gabazine purchased from MedChemExpress. Usage Cited in: Elife. 2024 May 29.
The peak ΔF/F in the Before RORR and RORR-Recovery stages with or without intracerebroventricular injection of Gabazine (4 μg/mL). Gabazine could increase the ΔF/F peak of calcium signaling in LCNE neurons.
Gabazine purchased from MedChemExpress. Usage Cited in: Elife. 2024 May 29.
The effects of intra-LC injection of Gabazine (4 μg/mL)and intra-VLPO injection of prazosin on the recovery time of midazolam. Microinjection of Gabazine into the LC could reduce the recovery time.
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bioRxiv
2023 Jul 22:2023.04.28.538437. PMID: 37163128 -
Oxid Med Cell Longev
Activation of TGR5 Ameliorates Streptozotocin-Induced Cognitive Impairment by Modulating Apoptosis, Neurogenesis, and Neuronal Firing. [Abstract]2022 Apr 15;2022:3716609. PMID: 35464765
Solvant et solubilité
H2O : 100 mg/mL (271.57 mM; Need ultrasonic)
DMSO : ≥ 75 mg/mL (203.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* 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.
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* 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.
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 (6.79 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 (6.79 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 7.14 mg/mL (19.39 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.7157 mL | 13.5785 mL | 27.1569 mL | 67.8923 mL |
| 5 mM | 0.5431 mL | 2.7157 mL | 5.4314 mL | 13.5785 mL | |
| 10 mM | 0.2716 mL | 1.3578 mL | 2.7157 mL | 6.7892 mL | |
| 15 mM | 0.1810 mL | 0.9052 mL | 1.8105 mL | 4.5262 mL | |
| 20 mM | 0.1358 mL | 0.6789 mL | 1.3578 mL | 3.3946 mL | |
| 25 mM | 0.1086 mL | 0.5431 mL | 1.0863 mL | 2.7157 mL | |
| 30 mM | 0.0905 mL | 0.4526 mL | 0.9052 mL | 2.2631 mL | |
| 40 mM | 0.0679 mL | 0.3395 mL | 0.6789 mL | 1.6973 mL | |
| 50 mM | 0.0543 mL | 0.2716 mL | 0.5431 mL | 1.3578 mL | |
| 60 mM | 0.0453 mL | 0.2263 mL | 0.4526 mL | 1.1315 mL | |
| 80 mM | 0.0339 mL | 0.1697 mL | 0.3395 mL | 0.8487 mL | |
| 100 mM | 0.0272 mL | 0.1358 mL | 0.2716 mL | 0.6789 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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