A neuropeptide with diverse biological activities
Etifoxine-13C-d3 is intended for use as an internal standard for the quantification of etifoxine 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 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.5
1.Hamon, A., Morel, A., Hue, B., et al.The modulatory effects of the anxiolytic etifoxine on GABAA receptors are mediated by the β subunitNeuropharmacology45(3)293-303(2003) 2.Verleye, M., Pansart, Y., and Gillardin, J.Effects of etifoxine on ligand binding to GABAA receptors in rodentsNeurosci. Res.44(2)167-172(2002) 3.Girard, C., Liu, S., Cadepond, F., et al.Etifoxine improves peripheral nerve regeneration and functional recoveryProc. Natl. Acad. Sci. USA105(51)20505-20510(2008) 4.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.21(6)457-470(2011) 5.Aouad, M., Zell, V., Juif, P.E., et al.Etifoxine analgesia in experimental monoarthritis: A combined action that protects spinal inhibition and limits central inflammatory processesPain155(2)403-412(2014)
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