| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
EC50: 0.2 μM (GABACreceptors)[1]
Muscimol is a potent orthosteric agonist of the GABAA receptor, binding to the same site as the endogenous neurotransmitter GABA. It acts as a selective agonist for GABAA (and also GABAC) receptors but has no activity at the GABAB receptor. It has an IC50 of 3.2 nM for the rat GABAA receptor. |
|---|---|
| ln Vitro |
In vitro, Muscimol is a potent agonist of the GABAA receptor, with reported EC50 values ranging from 1.4 uM to 28 uM depending on the receptor configuration and cell type. It also acts as an agonist at GABAC receptors. It fails to activate GABAB receptors, demonstrating its subtype selectivity.
|
| ln Vivo |
After being injected into the ventral prefrontal cortex (1 μL, 5 μg/μL; prefrontal cortex infusion), mycopolyl has an impact on prefrontal cortex function and reduces monkey performance on a counting test, but not when injected into the dorsal prefrontal cortex[2]. In the 10-second microdose group (62.5 or 125 µg/side), musclemol had no effect on suppression of noise stimulation, but it does affect microdose regulation in the anterior cingulate cortex (ACC)[3].
In vivo, Muscimol passes the blood-brain barrier (BBB) and has memory-disrupting effects. It is known to impair associative and memory functions and is used in research to produce a reversible decrease in neuronal activity in specific brain regions, mimicking an inhibitory lesion. It produces its effects by activating GABAA receptors, leading to neuronal hyperpolarization. |
| Enzyme Assay |
The non-cellular protocol for determining binding affinity for Muscimol is a radioligand competition assay using [3H]muscimol itself. Rat brain synaptic membranes are prepared and incubated with [3H]muscimol and varying concentrations of unlabeled test compounds (e.g., for competition studies) to determine the binding affinity of GABAA receptor ligands.
|
| Cell Assay |
N/A. Since Muscimol activates an ion channel directly, functional assays are best done in live cells. A standard cellular protocol uses Xenopus laevis oocytes injected with cRNA encoding human GABAA receptor subunits. Two-electrode voltage-clamp electrophysiology is used to record chloride currents. Increasing concentrations of Muscimol are applied, and the peak current amplitude is measured to determine the EC50.
|
| Animal Protocol |
Animal/Disease Models: Female rhesus monkeys (Macaca mulatta) (5 kg and 5.5 kg)[2]
Doses: 1 μL, 5 μg/μL Route of Administration: Implanted drug delivery tubes and infusion; single dose Experimental Results: Increased the error types and reaction time during the counting task. To study the effect of a localized “lesion”, a rat is stereotaxically implanted with a cannula into a specific brain region (e.g., the amygdala or hippocampus). After recovery, Muscimol (0.5-1 uL of a 0.5-1 ug/uL solution) is infused into the region. The animal then undergoes a behavioral test (e.g., fear conditioning or water maze) to assess the functional contribution of that brain region. |
| ADME/Pharmacokinetics |
Muscimol is known to permeate the blood-brain barrier (BBB). It is a psychoactive compound. Its ability to penetrate the BBB and its relatively high potency for the GABAA receptor is what makes it a potent central nervous system tool, as it can be administered systemically (though intracerebral infusion is more precise for acute effects).
|
| Toxicity/Toxicokinetics |
Muscimol is toxic (classified as Toxic F). It is a known neurotoxin and can cause severe CNS depression, hallucinations, and seizures at high doses. In experimental settings, its toxicity is managed by using localized, low-dose infusions into brain tissue. Its LD50 depends on the route of administration and species.
|
| References |
|
| Additional Infomation |
Muscimol is a cornerstone of GABAA research, often serving as the “gold standard” agonist in screening assays for new GABAA receptor modulators. It is also used as a positive control in functional electrophysiology experiments. Unlike benzodiazepines which are allosteric modulators, Muscimol directly opens the ion channel, making it an essential tool for defining orthosteric agonist activity.
|
| Molecular Formula |
C4H7CLN2O2
|
|---|---|
| Molecular Weight |
150.56
|
| Exact Mass |
150.02
|
| Elemental Analysis |
C, 31.91; H, 4.69; Cl, 23.55; N, 18.61; O, 21.25
|
| CAS # |
3579-03-1
|
| Related CAS # |
Muscimol;2763-96-4; 3579-03-1 (HCl); 18174-72-6 (HBr)
|
| PubChem CID |
77108154
|
| Appearance |
White to light yellow solid powder
|
| LogP |
1.341
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
9
|
| Complexity |
141
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=C(ONC1=O)CN.Cl
|
| InChi Key |
IIDOLBNZAZXSHC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C4H6N2O2.ClH/c5-2-3-1-4(7)6-8-3;/h1H,2,5H2,(H,6,7);1H
|
| Chemical Name |
5-(aminomethyl)-1,2-oxazol-3-one;hydrochloride
|
| Synonyms |
Muscimol hydrochloride; NSC-304080; Muscimol HCl; NSC-304,080; Agarin HCl; Agarin hydrochloride; NSC304080; NSC 304080; 18174-72-6; 5-(Aminomethyl)-3(2H)-isoxazolone hydrobromide; 3(2H)-Isoxazolone, 5-(aminomethyl)-, monohydrobromide; 5-(Aminomethyl)-3-isoxazolol monohydrochloride;
|
| HS Tariff Code |
2934.99.9001
|
| 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 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
|
|---|---|
| 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 | 6.6419 mL | 33.2094 mL | 66.4187 mL | |
| 5 mM | 1.3284 mL | 6.6419 mL | 13.2837 mL | |
| 10 mM | 0.6642 mL | 3.3209 mL | 6.6419 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
