产品描述: | Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents |
靶点: |
GABA Receptor;GABAReceptor |
体内研究: |
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. |
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. 3. Marc Verleye, et al. Differential effects of etifoxine on anxiety-like behaviour and convulsions in BALB/cByJ and C57BL/6J mice: any relation to overexpression of central GABAA receptor beta2 subunits? Eur Neuropsychopharmacol. 2011 Jun;21(6):457-70. |
溶解性: |
Soluble in DMSO、H2O |
保存条件: |
-20°C |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.965 ml |
14.826 ml |
29.652 ml |
5 mM |
0.593 ml |
2.965 ml |
5.93 ml |
10 mM |
0.297 ml |
1.483 ml |
2.965 ml |
50 mM |
0.059 ml |
0.297 ml |
0.593 ml |
|
注意: |
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