| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
The primary target of Etifoxine is the GABAA receptor. It acts as a positive allosteric modulator, selectively increasing GABA-induced currents in X. laevis oocytes expressing α1β2γ2 or α1β3γ2 receptors. It also inhibits the binding of the GABAA receptor agonist muscimol. By enhancing GABAergic transmission, it produces anxiolytic and anticonvulsant effects.
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| ln Vitro |
Etefosine (EFX) increases [3H]muscimol binding at equilibrium in a dose-dependent manner at concentrations between 10 and 300 μM (higher concentrations limit its solubility); at 300 μM, EFX 21 reaches 155± of its control value.
In vitro, Etifoxine is a positive allosteric modulator of GABAA receptors. It selectively increases GABA-induced currents in oocytes expressing α1β2γ2 or α1β3γ2. It increases NGF-induced neurite outgrowth in PC12 cells. It inhibits axonal growth. Its activity is characterized by its dual mechanism of action on GABAA receptor subtypes. |
| ln Vivo |
At micromolar doses, etifoxine competitively reduces [35S]TBPS binding in rat brain [1]. When compared to C57BL/6J mice, BALB/cByJ mice show more pronounced anxiolytic and anticonvulsant effects when exposed to etifoxine (3.125-50 mg/kg) [3].
In vivo, Etifoxine has anxiolytic-like activity in animal models. It increases the percentage of time spent in the open arms of the elevated plus maze in high-anxiety mice. It increases the seizure threshold in a mouse model of seizures induced by picrotoxin. It also increases the paw withdrawal threshold. It is used clinically as an anxiolytic in some countries. |
| Enzyme Assay |
For GABAA receptor functional assays, Xenopus laevis oocytes are injected with cRNA encoding the receptor subunits. Two-electrode voltage clamp is used to measure GABA-induced currents. Etifoxine is applied with GABA, and the potentiation of currents is measured. For binding assays, the compound's affinity for the receptor is measured using radioligand binding.
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| Cell Assay |
For cellular studies, neuronal cells (e.g., PC12 cells) are cultured. Etifoxine is dissolved in DMSO and diluted in culture medium. Cells are treated with the compound. Neurite outgrowth is measured by microscopy. For mechanistic studies, signaling pathways are analyzed by Western blot.
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| Animal Protocol |
Animal/Disease Models: Sixweeks old BALB/cByJ and C57BL/6J mice (20-25 g) [3].
Doses: 3.125-50 mg/kg. Route of Administration: intraperitoneal (ip) injection. Experimental Results: The 12.5 mg/kg dose of BALB/cByJ mice Dramatically increased arm open time compared to vehicle (p = 0.009), but had no effect in C57B/6J mice. BALB/cByJ mice demonstrated Dramatically (p < 0.012) lower plasma compound levels at 15 and 30 min compared with C57BL/6J mice. For in vivo efficacy studies, animal models of anxiety or epilepsy are used. Etifoxine is formulated in vehicle and administered intraperitoneally or orally. Behavior is assessed using the elevated plus maze, open field test, or other anxiety tests. Seizure threshold is determined by administering a convulsant and measuring latency to seizure. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for Etifoxine indicate that it is orally active. It has good oral bioavailability and can cross the blood-brain barrier. Its metabolism likely involves hepatic CYP450 enzymes. Its half-life and other PK parameters have been characterized in clinical studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Etifoxine show that it has a high LD50 in mice (12 g/kg orally). It is generally well-tolerated, but can cause side effects such as drowsiness and dizziness. As with all drugs, it should be used with caution.
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| References |
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| Additional Infomation |
Etefosine is a benzodiazepine. It is an anti-anxiety and anticonvulsant drug developed by Hearst Corporation in the 1960s. It is used to treat anxiety disorders and promote peripheral nerve healing. Although its effects are similar to benzodiazepines, it does not bind to benzodiazepine receptors. As an anti-anxiety drug, it is more effective than lorazepam and has fewer side effects. Etefosine has been associated with acute liver injury.
Etifoxine (CAS 21715-46-8) is a non-benzodiazepine anxiolytic and positive allosteric modulator of GABAA receptors. It has the molecular formula C₁₇H₁₇ClN₂O and a molecular weight of 300.78. It is used in some countries for anxiety disorders and is strictly for research use. |
| Molecular Formula |
C₁₇H₁₇CLN₂O
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|---|---|
| Molecular Weight |
300.78
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| Exact Mass |
300.102
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| CAS # |
21715-46-8
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| Related CAS # |
Etifoxine hydrochloride;56776-32-0;Etifoxine-d5;1346598-10-4
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| PubChem CID |
135413553
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
421.2±55.0 °C at 760 mmHg
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| Melting Point |
90-92
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| Flash Point |
208.5±31.5 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.601
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| LogP |
3.78
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
394
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IBYCYJFUEJQSMK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17ClN2O/c1-3-19-16-20-15-10-9-13(18)11-14(15)17(2,21-16)12-7-5-4-6-8-12/h4-11H,3H2,1-2H3,(H,19,20)
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| Chemical Name |
6-chloro-N-ethyl-4-methyl-4-phenyl-1H-3,1-benzoxazin-2-imine
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| Synonyms |
HOE 36-801HOE 36801 HOE-36801 HOE36801 etafenoxine Stresam
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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) |
DMSO : ~100 mg/mL (~332.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.31 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 (8.31 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 (8.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3247 mL | 16.6234 mL | 33.2469 mL | |
| 5 mM | 0.6649 mL | 3.3247 mL | 6.6494 mL | |
| 10 mM | 0.3325 mL | 1.6623 mL | 3.3247 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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