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...

Background To investigate the effects of benzodiazepine receptor agonists on cognitive function in patients with chronic insomnia. Method According to history taking hypnotic drugs, they were divided into no medication group (n = 62), benzodiazepines 57) and non-benzodiazepines 53); all subjects The Pittsburgh Sleep Quality Scale, Epworth Insomnia Severity Index used evaluate their sleep qualit...

The intraventricular administration of [3H-methyl]-methionine resulted in a steady increase in carboxyl-[3H]methylated protein formation in the brain of developing rats (2-42 days). The analysis by gel filtration on Sepharose-4B of Lubrol-Px-solubilized membrane proteins, including benzodiazepine receptor proteins, revealed co-migration of carboxyl-[3H]methylated and [3H]flunitrazepam-binding p...

gamma-Aminobutyric acid (GABA) and benzodiazepine receptors have been solubilized and purified by procedures such as gel filtration, ion-exchange, lectin, and affinity chromatographies. All of these procedures enhance the specific activity of each receptor to a similar extent. The drug specificities of [3H]muscimol and [3H]flunitrazepam binding sites are the same after extensive purification by...

The presence of specific benzodiazepine binding sites in the hearts of dogs and human beings was demonstrated in vivo by a noninvasive method, positron emission tomography (PET). An antagonist of the peripheral-type benzodiazepine binding site, PK 11195, was labeled with carbon-11, a short-lived positron emitter. When injected at high specific activity, 11C-PK 11195 was concentrated in the myoc...

Seizures induced by an acute pentylenetetrazole (50 mg/kg) injection were accompanied by a long-term (at 1-48 h, but not on day 7) decrease in the density (B(max)) of [3H]-diazepam binding to benzodiazepine receptors in rat cerebellar cortex with no change in affinity (K(d)). Kindling for 24 days by daily administrations of pentylenetetrazole (20 mg/kg) led to the same decrease in benzodiazepin...

In vitro effects of dihydroergotoxine, dihydroergosine, dihydroergotamine, alpha-dihydroergocriptine (ergot alkaloids), diazepam, methyl-beta-Carboline-3-carboxilate (beta-CCM), flumazenil (benzodiazepines), gamma-amino butyric acid (GABA) and thiopental (barbiturate) were studied on mouse brain (cerebrum minus cerebral cortex) benzodiazepine binding sites labeled with 3H-flunitrazepam. Specifi...