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etifor
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There are 6 letters in ETIFOR ( E1F4I1O1R1T1 )
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| Etifor might refer to |
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Etifoxine (INN, also known as etafenoxine; trade name Stresam) is an anxiolytic and anticonvulsant drug developed by Hoechst in the 1960s. It is sold in approximately 40 countries for anxiety disorders, without the sedation and ataxia associated with benzodiazepine drugs. It has similar anxiolytic effects to benzodiazepine drugs, but is structurally distinct and does not bind to the benzodiazepine receptor. It is as effective as lorazepam as an anxiolytic, but has fewer side effects. Etifoxine is not a scheduled drug in many countries in which it is sold and does not cause dependence or tolerance. Etifoxine is not approved by the U.S. Food and Drug Administration or the European Medicines Agency. * Etifoxine seems to have been mischaracterized in the 1960-70's as a mild or partial benzodiazepine, because of its lack of typical benzodiazepine side effects, like sedation and ataxia. Thus, it was deemed to be noncompetitive with benzodiazepine drugs of the time, like Valium, and not introduced into world markets. Not until the 2000s was it discovered that etifoxine worked through completely different mechanisms, i.e.. GABA(A) beta subtype selectivity and neurosteroid biosynthesis (purported to work through TSPO). Realization of the MOA has led to its investigation in a number of preclinical studies as an analgesic, anti-inflammatory and neuroprotectant. Recent publications have chronicled its efficacy as a microglia modulator in models of MS and ICH. * The original composition of matter patent for etifoxine has expired decades ago, however the S-enantiomer (US8110569 B2) and metabolically stabilized deuterium substituted variants have been recently identified in the patent literature (WO2016154039 A1). The deuterium variants retain the biological activity of etifoxine, but improve the pharmacokinetic profile, allowing less frequent and/or lower dosing than the original. |