Etifoxine hydrochloride

SKU: orb1219295

Description

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

Key Properties

• CAS Number: 56776-32-0
• MW: 337.24
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₈Cl₂N₂O
• SMILES: ClC1=CC=C2C(C(C3=CC=CC=C3)(C)OC(NCC)=N2)=C1.Cl
• Target: GABA
• Solubility: DMSO:50 mg/mL (148.26 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Etifoxine competitively inhibits [35S]TBPS binding with micromolar potency in rat brain. Etifoxine (3.125-50 mg/kg) exhibits more pronounced anxiolytic and anticonvulsant effects in the BALB/cByJ mice compared to the C57BL/6J mice. Animal model: Six-week old BALB/cByJ and C57BL/6J mice (20-25 g). 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HOE 36-801 hydrochloride

Quick Database Links

Gene Symbol

GABA