CAS号：56776-32-0
|
英文名称：Etifoxine hydrochloride
分子式
C17H18Cl2N2O
分子量
337
EINECS号
260-380-0
MDL
MFCD18086857
Smiles
InChIKey
盐酸依替福辛化学百科
基本信息
| 中文名称 | 盐酸艾替伏辛 |
| 英文名称 | 6-chloro-N-ethyl-4-methyl-4-phenyl-4H-3,1-benzoxazin-2-amine monohydrochloride |
| CAS号 | 56776-32-0 |
| 分子式 | C17H18Cl2N2O |
| 分子量 | 337.24362 |
| EINECS号 | 260-380-0 |
物化性质
| 熔点 | ND |
| 溶解度 | 二甲基亚砜：≥5mg/mL |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| 稳定性 | 吸湿性 |
安全信息
| 危险品标志 | Xn |
| 危险类别码 | 22 |
| WGK Germany | 3 |
生产及用途
Etifoxine hydrochloride是一个非苯二氮卓类的、具有 GABA 能的化合物，是 GABAA 受体亚基 α1β2γ2 和 α1β3γ2 的阳性变构调节剂。Etifoxine hydrochloride 在啮齿类动物中显示出抗焦虑和抗惊厥活性。
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 [
35
S]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. |
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