Etifoxine (Synonyms: 艾替伏辛; HOE 36-801)
目录号: PL04629 纯度: ≥99%
CAS No. :21715-46-8
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中文名称
Etifoxine
中文别名
艾替伏辛;2-乙基氨基-6-氯-4-甲基-4-苯基-4H-3,1-苯并恶嗪
英文名称
Etifoxine
英文别名
4H-3,1-Benzoxazin-2-amine,6-chloro-N-ethyl-4-methyl-4-phenyl-;Etifoxine;6-chloro-N-ethyl-4-methyl-4-phenyl-3,1-benzoxazin-2-amine;HOE 36-801;(6-chloro-4-methyl-4-phenyl-4H-benzo[d][1,3]oxazin-2-yl)-ethyl-amine;Etafenoxine;Etifoxin;Etifoxina [INN-Spanish];Etifoxina [Spanish];Etifoxinum [INN-Latin];Etifoxinum [Latin];rac-etifoxine
Cas No.
21715-46-8
分子式
C17H17N2OCl
分子量
300.78
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Etifoxine 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 在啮齿类动物中显示出抗焦虑和抗惊厥活性。
生物活性
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABA A receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
性状
Solid
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Etifoxine competitively inhibits [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.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Marc Verleye, et al. Effects of etifoxine on ligand binding to GABA(A) receptors in rodents. Neurosci Res. 2002 Oct;44(2):167-72.
[2]. Alain Hamon, et al. The modulatory effects of the anxiolytic etifoxine on GABA(A) receptors are mediated by the beta subunit. Neuropharmacology. 2003 Sep;45(3):293-303.
溶解度数据
In Vitro: DMSO : 100 mg/mL (332.47 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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