etifoxine

Etifoxine is a benzoxazine-class small molecule anxiolytic and anticonvulsant developed by Hoechst in the 1960s. It is primarily indicated for the short-term management of adjustment disorder with anxiety, such as stress-induced anxiety, and is also being studied for peripheral nerve healing and chemotherapy-induced pain[1][2][7]. Unlike benzodiazepines, etifoxine exerts its effects through a dual mechanism of action: - Direct allosteric modulation of Gamma-aminobutyric acid type A receptor (GABAA receptor) at the α+β− interface (distinct from the classical benzodiazepine site), preferentially potentiating α2β3γ2 and α3β3γ2 receptor subtypes[1][4]. - Indirect enhancement of GABAergic neurotransmission via stimulation of neurosteroid synthesis after binding to the mitochondrial translocator protein (TSPO), formerly known as the peripheral benzodiazepine receptor (PBR)[1][4][5]. This leads to increased production of neurosteroids like allopregnanolone, which further modulate GABAA receptors. Etifoxine has demonstrated neuroprotective, neuroplastic, and anti-inflammatory properties in addition to its anxiolytic effects[2][5]. It does not cause typical benzodiazepine side effects such as dependence or significant sedation[5].

Brand names

Stresam