The Non-Benzodiazepine Anxiolytic Drug Etifoxine Causes a Rapid, Receptor-Independent Stimulation of Neurosteroid Biosynthesis

The Non-Benzodiazepine Anxiolytic Drug Etifoxine Causes a Rapid, Receptor-Independent Stimulation of Neurosteroid Biosynthesis

Neurosteroids can modulate the activity of the GABAA receptors, and thus affect anxiety-like behaviors. The non-benzodiazepine anxiolytic compound etifoxine has been shown to increase neurosteroid concentrations in brain tissue but the mode of action of etifoxine on neurosteroid formation has not yet been elucidated. In the present study, we have thus investigated the effect and the mechanism o...

Modulation of GABAergic synaptic transmission by the non-benzodiazepine anxiolytic etifoxine.

We have investigated the effects of 2-ethylamino-6-chloro-4-methyl-4-phenyl-4H-3,1-benzoxazine hydrochloride (etifoxine) on GABA(A) receptor function. Etifoxine displaced [(35)S]TBPS (t-butylbicyclophosphorothionate) from GABA(A) receptors of rat cortical membranes with an IC(50) of 6.7+/-0.8 microM and [(3)H]PK11195 from peripheral (mitochondrial)-type benzodiazepine receptors (PBRs) of rat he...

Etifoxine for Pain Patients with Anxiety

Etifoxine (etafenoxine, Stresam®) is a non-benzodiazepine anxiolytic with an anticonvulsant effect. It was developed in the 1960s for anxiety disorders and is currently being studied for its ability to promote peripheral nerve healing and to treat chemotherapy-induced pain. In addition to being mediated by GABAAα2 receptors like benzodiazepines, etifoxine appears to produce anxiolytic effects d...

Neurosteroid Biosynthesis in the Brain of Amphibians

Amphibians have been widely used to investigate the synthesis of biologically active steroids in the brain and the regulation of neurosteroid production by neurotransmitters and neuropeptides. The aim of the present review is to summarize the current knowledge regarding the neuroanatomical distribution and biochemical activity of steroidogenic enzymes in the brain of anurans and urodeles. The d...

Receptor Occupancy of Non-Peptide CRF1 Antagonist DMP696: Correlation with Drug Exposure and Anxiolytic Efficacy