艾替伏辛
中文名称 | 艾替伏辛 |
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中文同义词 | 艾替伏辛;2-乙基氨基-6-氯-4-甲基-4-苯基-4H-3,1-苯并恶嗪;2-乙基氨基-6-氯-4-甲基-4-苯基-4H-3 |
英文名称 | Etifoxine |
英文同义词 | etafenoxine;36-801;6-Chloro-2-ethylamino-4-methyl-4-phenyl-4H-3,1-benzoxazine;Etifoxin;HOE-36801;HOE-36-801;2-Ethylamino-6-chloro-4-methyl-4-phenyl-4H-3,1-benzoxazine;Etifoxine |
CAS号 | 21715-46-8 |
分子式 | C17H17ClN2O |
分子量 | 300.78 |
EINECS号 | 630-330-6 |
相关类别 | 神经系统用药;离子通道;膜转运;膜转运/离子通道 |
Mol文件 | 21715-46-8.mol |
结构式 |
艾替伏辛 性质
熔点 | 90-92℃ |
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沸点 | 421.2±55.0 °C(Predicted) |
密度 | 1.1716 (rough estimate) |
蒸气压 | 0-1Pa at 20-25℃ |
折射率 | 1.5800 (estimate) |
储存条件 | Store at -20°C |
溶解度 | DMSO:60.0(最大浓度 mg/mL);199.47(最大浓度 mM) DMF:30.0(最大浓度 mg/mL);99.74(最大浓度 mM) DMF:PBS ( pH 7.2) (1:8):0.1(最大浓度 mg/mL);0.33(最大浓度 mM) 乙醇:20.0(最大浓度 mg/mL);66.49(最大浓度 mM) |
形态 | 固体:颗粒/粉末 |
酸度系数(pKa) | 4.89±0.40(Predicted) |
颜色 | 浅黄至黄色 |
LogP | 4.09-4.52 at 21-25℃ and pH7 |
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 injection. |
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. |
安全信息
毒性 | LD50 orally in mice: 12 g/kg (Hoffmann) |
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-16579A | 艾替伏辛 Etifoxine | 21715-46-8 | 5mg | 780元 |
2024/04/30 | HY-16579A | 艾替伏辛 Etifoxine | 21715-46-8 | 10mM * 1mLin DMSO | 858元 |