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| 10mg |
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| 25mg |
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| 50mg |
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Etifoxine (HOE-36801) and etafenoxine, is a non-benzodiazepine GABAergic anxiolytic and anticonvulsant drug developed by Hoechst in the 1960s, and sold in approximately 40 countries for anxiety disorders, without the sedation and ataxia associated with benzodiazepine drugs. Unlike benzodiazepines, etifoxine appears to produce its anxiolytic effects by binding to β2 and β3 subunits of the GABAA receptor complex, and so is acting at a different target site to benzodiazepines, although the physiological effect that is produced is similar to that of benzodiazepines.
| 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.
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| 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].
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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. |
| References |
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| Additional Infomation |
Etifoxine is a benzoxazine.
Etifoxine is an anxiolytic and anticonvulsant drug developed by Hoechst in the 1960s. It is used in anxiety disorders and to promote peripheral nerve healing. It does not bind to the benzodiazepine receptor though the effects are similar to that of benzodiazepines. It is more effective than lorazepam as an anxiolytic, and has fewer side effects. Etifoxine has been associated with acute liver injury. |
| 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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