Etifoxine(HOE 36-801)是GABAA受体增强剂,倾向作用于含β2或β3亚基的GABAA受体。
Cas No. | 21715-46-8 |
别名 | 艾替伏辛,HOE 36-801 |
Canonical SMILES | ClC1=CC=C2C(C(C3=CC=CC=C3)(C)OC(NCC)=N2)=C1 |
分子式 | C17H17ClN2O |
分子量 | 300.78 |
溶解度 | DMSO: 100 mg/mL (332.47 mM) |
储存条件 | Store at -20°C |
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(HOE 36-801) 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. [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;2
[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. |