Etifoxine hydrochloride 是一种非苯二氮卓类 GABA 能化合物，是含有 α1β2γ2 和 α1β3γ2 亚基的 GABAA 受体的正变构调节剂。
| Cas No. | 56776-32-0 |
| 别名 | 盐酸艾替伏辛,Stresam;HOE 36-801 |
| 化学名 | 6-chloro-N-ethyl-4-methyl-4-phenyl-3,1-benzoxazin-2-amine;hydrochloride |
| Canonical SMILES | CCNC1=NC2=C(C=C(C=C2)Cl)C(O1)(C)C3=CC=CC=C3.Cl |
| 分子式 | C17H18Cl2N2O |
| 分子量 | 337.24 |
| 溶解度 | ≥ 33.7 mg/mL in DMSO with gentle warming, ≥ 48.1 mg/mL in EtOH with gentle warming, ≥ 15.49 mg/mL in Water with gentle warming |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Etifoxine hydrochloride (HOE 36-801 hydrochlorid) is potentiator of GABAA receptor function in cultured neurons. Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. IC50 value:Target: GABAA receptorEtifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration. References:
[1]. Verleye M, Dumas S, Heulard I, 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.
[2]. Bourin M, Hascot M. Implication of 5-HT2 receptor subtypes in the mechanism of action of the GABAergic compound etifoxine in the four-plate test in Swiss mice. Behav Brain Res. 2010 Apr 2;208(2):352-8.
[3]. Gee KW, Tran MB, Hogenkamp DJ, et al. Limiting activity at beta1-subunit-containing GABAA receptor subtypes reduces ataxia. J Pharmacol Exp Ther. 2010 Mar;332(3):1040-53.
[4]. Aouad M, Charlet A, Rodeau JL, et al. Reduction and prevention of vincristine-induced neuropathic pain symptoms by the non-benzodiazepine anxiolytic etifoxine are mediated by 3alpha-reduced neurosteroids. Pain. 2009 Dec 15;147(1-3):54-9.
[5]. Girard C, Liu S, Cadepond F, et al. Etifoxine improves peripheral nerve regeneration and functional recovery. Proc Natl Acad Sci U S A. 2008 Dec 23;105(51):20505-10. |
