Etifoxine hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

依替福辛是一种抗焦虑和抗惊厥化合物。与苯二氮卓类化合物不同，依托替福辛似乎通过与 GABAA 受体复合物的 β2 和 β3 亚基结合来产生抗焦虑作用，因此作用于与苯二氮卓类化合物不同的靶位点，尽管产生的生理作用与苯二氮卓类化合物相似。

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.

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.

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.

HOE 36-801 hydrochloride

Others

Other Targets

GABA

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56776-32-0

337.24

C17H18Cl2N2O

>98% (HPLC)

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

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

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(-20℃)

With Ice Pack

≥ 2 years