| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 1g | |||
| Other Sizes |
| Targets |
Muscimol HBr targets the GABAA receptor, a ligand-gated ion channel that mediates fast inhibitory neurotransmission in the central nervous system. GABA is the primary inhibitory neurotransmitter in the mammalian brain. Muscimol acts as a potent and selective agonist, binding to the same site as GABA and activating the receptor. This leads to an influx of chloride ions into the neuron, causing hyperpolarization and reducing neuronal excitability.
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| ln Vitro |
In vitro, muscimol HBr is a standard agonist used to study GABAA receptor function. It is used in receptor binding assays to determine the affinity of other compounds for GABAA receptors. In electrophysiological studies, muscimol is used to activate GABAA receptors and measure chloride currents. Its effects are blocked by competitive antagonists like bicuculline. Its potency and selectivity make it a superior tool compared to GABA itself.
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| ln Vivo |
In vivo, muscimol HBr produces effects consistent with enhanced GABAergic inhibition. When administered systemically or directly into the brain, it can induce sedation, muscle relaxation, hypothermia, and ataxia. At higher doses, it can cause profound central nervous system depression. These effects are due to its potent activation of GABAA receptors. Muscimol is used in research to study the role of GABAergic transmission in various behaviors and neurological conditions.
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| Enzyme Assay |
In vitro receptor binding assays for muscimol HBr are performed using membrane preparations from brain tissue or cells expressing GABAA receptors. A radiolabeled agonist, such as [³H]-muscimol itself, is used as a tracer. Membranes are incubated with the radioligand and varying concentrations of unlabeled muscimol. The amount of bound radioligand is measured, and the compound's affinity (Ki) is determined. Electrophysiological assays, such as patch-clamp, are used to measure the functional activation of GABAA receptors.
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| Cell Assay |
For cell-based assays, neurons or cells expressing GABAA receptors are cultured in standard media. Cells are seeded in multi-well plates and treated with muscimol HBr at various concentrations. The activation of GABAA receptors is measured by assessing changes in intracellular chloride levels using fluorescent dyes, or by measuring membrane potential. The effects can be blocked by antagonists like bicuculline. All experiments include appropriate vehicle controls.
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| Animal Protocol |
In vivo studies with muscimol HBr are conducted in animal models to study the role of GABAergic neurotransmission. The compound is typically administered via intracerebroventricular (ICV) injection or directly into specific brain regions to avoid peripheral effects. Behavioral tests, such as the open field test, elevated plus maze, and rotarod test, are used to assess its effects on anxiety, locomotion, and motor coordination. All procedures must be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
Muscimol HBr is a small, zwitterionic molecule that does not readily cross the blood-brain barrier. Therefore, it is often administered directly into the brain for in vivo studies. Its pharmacokinetic properties are well-characterized in the literature. It is typically stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
Toxicity Summary
Musciclovir is a potent GABAA receptor agonist that activates receptors for GABA, the brain's primary inhibitory neurotransmitter. Musciclovir binds to the same binding site on the GABAA receptor complex as GABA itself, unlike other GABAergic drugs (such as barbiturates and benzodiazepines) which bind to different regulatory sites. GABAA receptors are widely distributed throughout the brain; therefore, when musciclovir is administered, it alters neuronal activity in multiple regions, including the cerebral cortex, hippocampus, and cerebellum. However, although musciclovir is generally considered a selective GABAA receptor agonist, it is also a potent partial agonist of GABAC receptors, thus its effects result from the combined action of two targets. (L1142) Toxicity Data LD50: 3.8 mg/kg (subcutaneous injection, mouse) (L1142) LD50: 2.5 mg/kg (intraperitoneal injection, mouse) (L1142) LD50: 4.5 mg/kg (intravenous injection, rat) (L1142) LD50: 45 mg/kg (oral administration, rat) (L1142) Muscimol is a potent neurotoxin. Overdose can lead to severe central nervous system depression, respiratory failure, and death. It is for research use only and is not for human consumption. Appropriate safety precautions must be taken when handling this compound. |
| Additional Infomation |
Muscimol (also known as fasciolidin or leopard antagonist) is the main psychoactive alkaloid found in various Amanita mushrooms. Unlike psilocybin, a tryptophan-like substance, fasciolidin is a potent and selective agonist of the GABAA receptor. Amanita muscaria contains two main active ingredients: isopentenyl acid and its derivative fasciolidin. Fascin is a product of the decarboxylation or drying of isopentenyl acid and is believed to be up to ten times more potent than isopentenyl acid. (L1142)
Muscimol HBr is a research-grade chemical probe, and its primary application is in the study of GABAergic neurotransmission. It is a potent and selective agonist of the GABAA receptor. The compound is not an approved drug and is not used therapeutically. It is commercially available from various chemical suppliers for research purposes only. Its use has been fundamental to our understanding of inhibitory signaling in the brain. |
| Molecular Formula |
C4H7BRN2O2
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|---|---|
| Molecular Weight |
195.01
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| Exact Mass |
193.969
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| Elemental Analysis |
C, 24.64; H, 3.62; Br, 40.97; N, 14.36; O, 16.41
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| CAS # |
18174-72-6
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| Related CAS # |
3579-03-1 (HCl); 2763-96-4; 18174-72-6 (HBr)
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| PubChem CID |
205536
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.291 g/cm3
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| Boiling Point |
325ºC at 760 mmHg
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| Melting Point |
172ºC
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| Flash Point |
150.4ºC
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| Vapour Pressure |
0.0463mmHg at 25°C
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| LogP |
1.497
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
9
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| Complexity |
141
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Br.NCC1ONC(=O)C=1
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| InChi Key |
OPZOJWHOZRKYQX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C4H6N2O2.BrH/c5-2-3-1-4(7)6-8-3;/h1H,2,5H2,(H,6,7);1H
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| Chemical Name |
5-(aminomethyl)-1,2-oxazol-3-one;hydrobromide
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| Synonyms |
Agarin hydrobromide; Muscimol HBr; Muscimol hydrobromide; NSC-304080; NSC-304,080; Agarin hydrobromide; Agarin HBr; NSC304080; NSC 304080; 18174-72-6; 5-(Aminomethyl)-3(2H)-isoxazolone hydrobromide; 3(2H)-Isoxazolone, 5-(aminomethyl)-, monohydrobromide; 5-(Aminomethyl)-3-isoxazolol monohydrobromide; Muscimol 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.1279 mL | 25.6397 mL | 51.2794 mL | |
| 5 mM | 1.0256 mL | 5.1279 mL | 10.2559 mL | |
| 10 mM | 0.5128 mL | 2.5640 mL | 5.1279 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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