Etifoxine

Etifoxine is a positive allosteric modulator of alpha1beta2gamma2 and alpha1beta3gamma2 subunit-containing GABAA receptors. It selectively increases GABA-induced currents in X. laevis oocytes expressing alpha1beta2gamma2 or alpha1beta3gamma2 over alpha1beta1gamma2 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. It increases NGF-induced neurite outgrowth in PC12 cells when used at a concentration of 20 µM. 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. It increases the seizure threshold in a mouse model of seizures induced by picrotoxin (Cay-20771) with a minimum effective dose (MED) of 75 mg/kg. 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.Formal Name: 6-chloro-N-ethyl-4-methyl-4-phenyl-4H-3,1-benzoxazin-2-amine. CAS Number: 21715-46-8. Synonyms: Etafenoxine, HOE 36-801. Molecular Formula: C17H17ClN2O. Formula Weight: 300.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:8): 0.1 mg/ml, DMSO: 20 mg/ml, Ethanol: 20 mg/ml. lambdamax: 275 nm. SMILES: CCNC(OC1(C2=CC=CC=C2)C)=NC3=C1C=C(Cl)C=C3. InChi Code: InChI=1S/C17H17ClN2O/c1-3-19-16-20-15-10-9-13(18)11-14(15)17(2,21-16)12-7-5-4-6-8-12/h4-11H,3H2,1-2H3,(H,19,20). InChi Key: IBYCYJFUEJQSMK-UHFFFAOYSA-N.