1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. Etifoxine hydrochloride

Etifoxine hydrochloride (Synonyms: HOE 36-801 hydrochloride)

Cat. No.: HY-16579 Purity: 99.96%
Handling Instructions

Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.

For research use only. We do not sell to patients.

Etifoxine hydrochloride Chemical Structure

Etifoxine hydrochloride Chemical Structure

CAS No. : 56776-32-0

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10 mM * 1 mL in DMSO USD 77 In-stock
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50 mg USD 340 In-stock
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Description

Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].

In Vitro

Etifoxine (EFX), at concentrations ranging from 10 to 300 μM (higher concentrations limited its solubility), produces a dose-dependent increase in the [3H]muscimol binding at equilibrium, to 155±2% of its control value at 300 μM EFX[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Etifoxine competitively inhibits [35S]TBPS binding with micromolar potency in rat brain[1].
Etifoxine (3.125-50 mg/kg) exhibits more pronounced anxiolytic and anticonvulsant effects in the BALB/cByJ mice compared to the C57BL/6J mice[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week old BALB/cByJ and C57BL/6J mice (20-25 g)[3].
Dosage: 3.125-50 mg/kg.
Administration: Intraperitoneal inhection.
Result: Significantly increased the amount of time spent on the open arms at the 12.5 mg/kg dose when compared to vehicle (p = 0.009) in BALB/cByJ mice but produced no effect in C57B/6J mice.
BALB/cByJ mice compared with C57BL/6J mice exhibited significantly (p < 0.012) lower plasma levels of the compound at 15 and 30 min.
Clinical Trial
Molecular Weight

337.24

Formula

C₁₇H₁₈Cl₂N₂O

CAS No.

56776-32-0

SMILES

ClC1=CC=C2C(C(C3=CC=CC=C3)(C)OC(NCC)=N2)=C1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (148.26 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9652 mL 14.8262 mL 29.6525 mL
5 mM 0.5930 mL 2.9652 mL 5.9305 mL
10 mM 0.2965 mL 1.4826 mL 2.9652 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.96%

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Keywords:

EtifoxineHOE 36-801GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorAnxiolyticadjustmentdisorderTBPSInhibitorinhibitorinhibit

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Etifoxine hydrochloride
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