A positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors; selectively increases GABA-induced currents in X. laevis oocytes expressing α1β2γ2 or α1β3γ2 over α1β1γ2 subunit-containing receptors at 20 µM; inhibits muscimol binding in rat corticol membranes (Kd = 23 nM in a radioligand binding assay); increases NGF-induced neurite outgrowth in PC12 cells at 20 µM; increases the percentage of time spent in the open arms of the elevated plus maze in high-anxiety BALB/cByJ

Etifoxine – 25 mg

Brand:
Cayman
CAS:
21715-46-8
Storage:
-20
UN-No:
Non-Hazardous - /

Etifoxine is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors.{26117} 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.{53410} It increases NGF-induced neurite outgrowth in PC12 cells when used at a concentration of 20 µM.{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}  

 

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A positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors; selectively increases GABA-induced currents in X. laevis oocytes expressing α1β2γ2 or α1β3γ2 over α1β1γ2 subunit-containing receptors at 20 µM; inhibits muscimol binding in rat corticol membranes (Kd = 23 nM in a radioligand binding assay); increases NGF-induced neurite outgrowth in PC12 cells at 20 µM; 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 at 12.5 mg/kg; increases the seizure threshold in a mouse model of seizures induced by picrotoxin (MED = 75 mg/kg); increases the paw withdrawal threshold on the ipsilateral side in a rat model of rheumatoid arthritis induced by complete Freund’s adjuvant at 50 mg/kg

Formal name: 6-chloro-N-ethyl-4-methyl-4-phenyl-4H-3, 1-benzoxazin-2-amine

Synonyms:  Etafenoxine|HOE 36-801

Molecular weight: 300.8

CAS: 21715-46-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation||Product Type|Biochemicals|Receptor Pharmacology||Research Area|Cell Biology|Cell Signaling|Growth Factor Receptors||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Seizure Disorders

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