Etifoxine Hydrochloride - CAS 56776-32-0
Catalog number: 56776-32-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
GABA Receptor
Etifoxine Hydrochloride is Potentiator of GABAA receptor with anxiolytic and anticonvulsant activity.
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White Solid
6-Chloro-N-ethyl-4-methyl-4-phenyl-4H-3,1-benzoxazin-2-amine Hydrochloride; 2-Ethylamino-6-chloro-4-methyl-4-phenyl-4H-3,1-benzoxazine Hydrochloride
Soluble in DMSO
Store at -20 °C
Psychotropic agent with anxiolytic and anticonvulsant activity
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Melting Point:
133-135 °C
Canonical SMILES:
Current Developer:
1.Etifoxine versus alprazolam for the treatment of adjustment disorder with anxiety: a randomized controlled trial.
Stein DJ1. Adv Ther. 2015 Jan;32(1):57-68. doi: 10.1007/s12325-015-0176-6. Epub 2015 Jan 27.
BACKGROUND: Adjustment disorder with anxiety (ADWA) is a highly prevalent condition, particularly in primary care practice. There are relatively few systematic treatment trials in the area of ADWA, and there are few data on predictors of treatment response. Etifoxine is a promising agent insofar as it is not associated with dependence, but in primary care settings benzodiazepines continue to be frequently prescribed for psychiatric symptoms. A randomized controlled trial of etifoxine versus alprazolam for ADWA was undertaken, focusing on efficacy and safety measures, and including an investigation of predictors of clinical response.
2.A microPET comparison of the effects of etifoxine and diazepam on [(11)C]flumazenil uptake in rat brains.
Bouillot C1, Bonnefoi F1, Liger F1, Zimmer L2. Neurosci Lett. 2016 Jan 26;612:74-9. doi: 10.1016/j.neulet.2015.11.042. Epub 2015 Nov 28.
Using positron emission tomography (PET), the present study assessed the binding of [(11)C]flumazenil to GABA-A receptors in anesthetized rats following a single intravenous injection of an active dose of either etifoxine (25mg/kg) or diazepam (1mg/kg), which are both anxiolytic drugs. [(11)C]flumazenil binding was measured in five discrete brain structures, namely the caudate putamen, hippocampus, cerebellum, occipital cortex and parietal cortex. As expected, diazepam injection produced a significant decrease in [(11)C]flumazenil binding, which was interpreted as benzodiazepine GABA-A receptor occupancy, whereas etifoxine increased the binding of [(11)C]flumazenil. This first use of in vivo imaging after etifoxine administration revealed the activated binding pattern of [(11)C]flumazenil and highlighted the pharmacological differences between etifoxine and benzodiazepines. Using the same [(11)C]flumazenil radiotracer, PET neuroimaging could be applied to larger animals and, ultimately, to human subjects, thus providing new perspectives for better defining the molecular pharmacology of etifoxine.
3.The non-benzodiazepine anxiolytic drug etifoxine causes a rapid, receptor-independent stimulation of neurosteroid biosynthesis.
do Rego JL1, Vaudry D2, Vaudry H2. PLoS One. 2015 Mar 18;10(3):e0120473. doi: 10.1371/journal.pone.0120473. eCollection 2015.
Neurosteroids can modulate the activity of the GABAA receptors, and thus affect anxiety-like behaviors. The non-benzodiazepine anxiolytic compound etifoxine has been shown to increase neurosteroid concentrations in brain tissue but the mode of action of etifoxine on neurosteroid formation has not yet been elucidated. In the present study, we have thus investigated the effect and the mechanism of action of etifoxine on neurosteroid biosynthesis using the frog hypothalamus as an experimental model. Exposure of frog hypothalamic explants to graded concentrations of etifoxine produced a dose-dependent increase in the biosynthesis of 17-hydroxypregnenolone, dehydroepiandrosterone, progesterone and tetrahydroprogesterone, associated with a decrease in the production of dihydroprogesterone. Time-course experiments revealed that a 15-min incubation of hypothalamic explants with etifoxine was sufficient to induce a robust increase in neurosteroid synthesis, suggesting that etifoxine activates steroidogenic enzymes at a post-translational level.
4.Characterization of the fast GABAergic inhibitory action of etifoxine during spinal nociceptive processing in male rats.
Juif PE1, Melchior M1, Poisbeau P2. Neuropharmacology. 2015 Apr;91:117-22. doi: 10.1016/j.neuropharm.2014.12.022. Epub 2014 Dec 26.
Etifoxine (EFX) is a non-benzodiazepine anxiolytic which potentiate GABAA receptor (GABAAR) function directly or indirectly via the production of 3α-reduced neurosteroids. The later effect is now recognized to account for the long-term reduction of pain symptoms in various neuropathic and inflammatory pain models. In the present study, we characterized the acute antinociceptive properties of EFX during spinal pain processing in naive and monoarthritic rats using in vivo electrophysiology. The topical application of EFX on lumbar spinal cord segment, at concentrations higher than 30 μM, reduced the excitability of wide dynamic range neurons receiving non-nociceptive and nociceptive inputs. Windup discharge resulting from the repetitive stimulation of the peripheral receptive field, and recognized as a short-term plastic process seen in central nociceptive sensitization, was significantly inhibited by EFX at these concentrations. In good agreement, mechanical nociceptive thresholds were also significantly increased following an acute intrathecal injection of EFX.
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CAS 56776-32-0 Etifoxine Hydrochloride

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