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 a1B2y2 and a1B3y2 subunit-containing GABAA receptors.{26117} It selectively increases GABA-induced currents in X. laevis oocytes expressing a1B2y2 or a1B3y2 over a1B1y2 subunit-containing receptors at 20 uM. 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.{53410} It increases NGF-induced neurite outgrowth in PC12 cells when used at a concentration of 20 uM.{26118} 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.{53411} 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.{53410} 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.{53412}
1 mg
Cayman Chemical
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