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Etifoxine-13C-d3 is intended for use as an internal standard for the quantification of etifoxine (Item No. 15999) by GC- or LC-MS. Etifoxine is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors.1 It selectively increases GABA-induced currents in X. laevis oocytes expressing α1β2γ2 or α1β3γ2 over α1β1γ2 subunit-containing receptors at 20 µM. Etifoxine inhibits binding of the GABAA receptor agonist muscimol in rat corticol membranes with a Kd value of 23 nM in a radioligand binding assay.2 It increases NGF-induced neurite outgrowth in PC12 cells when used at a concentration of 20 µM.3 Etifoxine (12.5 mg/kg, i.p.) increases the percentage of time spent in the open arms of the elevated plus maze in high-anxiety BALB/cByJ, but not C57BL/6, mice, indicating anxiolytic-like activity.4 It increases the seizure threshold in a mouse model of seizures induced by picrotoxin (Item No. 20771) with a minimum effective dose (MED) of 75 mg/kg.2 Etifoxine (50 mg/kg, i.p.) also increases the paw withdrawal threshold on the ipsilateral side in a rat model of rheumatoid arthritis induced by complete Freund's adjuvant.5WARNING This product is not for human or veterinary use. | [References]
[1] ALAIN HAMON . The modulatory effects of the anxiolytic etifoxine on GABAA receptors are mediated by the β subunit[J]. Neuropharmacology, 2003, 45 3: Pages 293-303. DOI: 10.1016/s0028-3908(03)00187-4
[2] MARC VERLEYE Jean M G Yannick Pansart. Effects of etifoxine on ligand binding to GABAA receptors in rodents[J]. Neuroscience Research, 2002, 44 2: Pages 167-172. DOI: 10.1016/s0168-0102(02)00121-9
[3] CHRISTELLE GIRARD. Etifoxine improves peripheral nerve regeneration and functional recovery.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2008, 105 51: 20505-20510. DOI: 10.1073/pnas.0811201106
[4] MARC VERLEYE . 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?[J]. European Neuropsychopharmacology, 2011, 21 6: Pages 457-470. DOI: 10.1016/j.euroneuro.2010.09.008
[5] MAYA AOUAD. Etifoxine analgesia in experimental monoarthritis: A combined action that protects spinal inhibition and limits central inflammatory processes[J]. PAIN®, 2014, 155 2: Pages 403-412. DOI: 10.1016/j.pain.2013.11.003 |
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