Etifoxine

Etifoxine is a positive allosteric modulator of α₁β₂γ₂ and α₁β₃γ₂ subunit-containing GABA_A 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 GABA_A receptor agonist muscimol in rat corticol membranes with a K_d 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.⁵

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