| Size | Price | Stock | Qty |
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| 5mg |
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| 50mg |
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| 100mg |
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| Targets |
Gabazine targets GABAA receptors as a selective and competitive antagonist. It has an IC50 of ~0.2 μM for GABA receptors. Gabazine binds to the GABA recognition site of the receptor-channel complex and acts as an allosteric inhibitor of channel opening. It displaces [³H]-GABA from rat brain membranes with a Ki of 150 nM. Gabazine is effective against GABAA receptor isoforms from mice, rats, and humans.
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| ln Vitro |
Two drugs that are thought to be competitive inhibitors of GABA binding to GABAA receptors are bucculline and gabazine (SR 95531). When it comes to stopping GABA-generated currents, gabazine works better than bicuculline. Its IC50 is roughly 0.2 μM, and for currents induced by 3 μM GABA, it has a Hill coefficient of 1.0. Gabazine decreased the current induced by 10 μM alphaxalone by roughly 30% when it came to receptors with the wild-type β2 subunit. The gabazine concentration (~0.2 μM) required to generate half of the largest block. Additionally, only a partial current blockage gated by 300 μM pentobarbital was induced by gabazine. Once more, the maximum reduction is roughly 30%, and roughly 0.15 μM of gabazine is needed to form half of the largest block [1].
In vitro, gabazine is a selective and competitive antagonist of GABAA receptor with an IC50 of ~0.2 μM for GABA receptor. It displaces [³H]-GABA from rat brain membranes with a Ki of 150 nM. Gabazine binds to the GABA recognition site of the receptor-channel complex and acts as an allosteric inhibitor of channel opening. Its antagonistic activity has been characterized in electrophysiological studies using recombinant GABAA receptors expressed in Xenopus oocytes or mammalian cells. |
| ln Vivo |
In vivo, gabazine is effective against GABAA receptor isoforms from mice, rats, and humans. It is used in scientific research and has no role in medicine, as it would be expected to produce convulsions if used in humans. Gabazine is used as a research tool to study GABAergic neurotransmission and the role of GABAA receptors in various physiological and pathological processes.
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| Enzyme Assay |
In non-cell-based receptor binding assays, gabazine's affinity for GABAA receptors is evaluated using radioligand competition binding experiments. Membrane preparations from rat brain or cells expressing recombinant GABAA receptors are incubated with a radiolabeled GABAA receptor ligand (such as [³H]GABA or [³H]muscimol) and varying concentrations of gabazine. After incubation, bound and free radioligand are separated by filtration, and radioactivity is measured. Competition curves are generated to determine IC50 and Ki values. These assays have established gabazine's Ki of 150 nM for rat brain membranes.
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| Cell Assay |
In vitro cellular assays for gabazine involve measuring its antagonist activity at GABAA receptors in cultured cells. Cells expressing recombinant GABAA receptors are treated with gabazine in the presence of GABA, and receptor activation is assessed using patch-clamp electrophysiology, fluorescence-based membrane potential assays, or calcium imaging. The compound's ability to inhibit GABA-evoked currents is quantified. Its effects on neuronal excitability and synaptic transmission are assessed in neuronal cultures.
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| Animal Protocol |
In vivo animal studies for gabazine have been conducted in rodent models to assess its effects on GABAergic neurotransmission and behavior. The compound is typically administered via intracerebroventricular or systemic routes, and its effects on seizure susceptibility, anxiety, and motor function are assessed. Gabazine produces convulsions due to its antagonism of GABAA receptors. It is used as a research tool to study GABAergic function.
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| ADME/Pharmacokinetics |
Gabazine has a molecular weight of 368.23 and a molecular formula of C15H15BrN4O3. It is a selective and competitive antagonist of GABAA receptor with an IC50 of ~0.2 μM. The compound is typically stored as a powder at -20°C for long-term stability. In solvent, it can be stored at -80°C for extended periods.
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| Toxicity/Toxicokinetics |
Gabazine is a research compound and is not intended for human use. It would be expected to produce convulsions if used in humans. The compound should be handled with appropriate safety precautions, including the use of personal protective equipment. It should be stored and handled in accordance with standard laboratory safety guidelines for neuroactive compounds.
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| References | |
| Additional Infomation |
Gabazine (SR-95531) is a selective and competitive antagonist at GABAA receptors with an IC50 of ~0.2 μM. It binds to the GABA recognition site of the receptor-channel complex and acts as an allosteric inhibitor of channel opening. Gabazine displaces [³H]-GABA from rat brain membranes with a Ki of 150 nM. It is used in scientific research to study GABAergic neurotransmission and is not an approved drug.
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| Molecular Formula |
C15H17N3O3
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| Molecular Weight |
287.31378
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| Exact Mass |
367.053
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| CAS # |
104104-50-9
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| PubChem CID |
107895
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| Appearance |
White to off-white solid powder
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| Boiling Point |
474.4ºC at 760 mmHg
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| Melting Point |
200 ºC (ethanol )
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| Flash Point |
240.7ºC
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| Vapour Pressure |
8.33E-10mmHg at 25°C
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
451
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GFZHNFOGCMEYTA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H17N3O3.BrH/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20;/h4-9,16H,2-3,10H2,1H3,(H,19,20);1H
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| Chemical Name |
4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl]butanoic acid;hydrobromide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~271.57 mM)
DMSO : ≥ 75 mg/mL (~203.68 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 7.14 mg/mL (19.39 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4806 mL | 17.4028 mL | 34.8056 mL | |
| 5 mM | 0.6961 mL | 3.4806 mL | 6.9611 mL | |
| 10 mM | 0.3481 mL | 1.7403 mL | 3.4806 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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