BACKGROUND/AIMS To measure cerebral benzodiazepine receptor binding using (11)C-flumazenil positron emission tomography in patients with stable chronic hepatic encephalopathy, who were also characterised by proton magnetic resonance spectroscopy. METHODS Six abstinent patients of mean age 61 years with alcohol related cirrhosis and grade I-II hepatic encephalopathy and 11 matched healthy volu...

The GABA(A) receptor mutation gamma(2)R43Q causes absence epilepsy in humans. Homology modeling suggests that gamma(2)Arg43, gamma(2)Glu178, and beta(2)Arg117 participate in a salt-bridge network linking the gamma(2) and beta(2) subunits. Here we show that several mutations at these locations exert similar long-distance effects on other intersubunit interfaces involved in GABA and benzodiazepin...

The purpose of this study was to investigate the anxiolytic effects of xanthohumol, a component of Humulus lupulus (hops), and its potential interaction with the benzodiazepine binding site on the y-aminobutyric acid (GABAA) receptor in the male Sprague-Dawley rat. This was a prospective, randomized, between-subjects experimental study. Fifty-five rats were assigned to 1 Sof 5 groups with 11 ra...

In this study, we compared the effects of Type I benzodiazepine receptor-selective agonists (zolpidem, quazepam) and Type I/II non-selective agonists (zopiclone, triazolam, nitrazepam) with either an ultra-short action (zolpidem, zopiclone, triazolam) or long action (quazepam, nitrazepam) on motor coordination (rota-rod test) and muscle relaxation (traction test) following the recovery from thi...

The effects of the benzodiazepine receptor antagonists flumazenil (10, 20, and 30 mglkg) and CGS 8216 (10, 20, and 30 mglkg), the benzodiazepine receptor inverse-agonist methyl {3-carboline3-carboxylate ({3-CCM; 0.3, 0.6, and 1.0 mglkg), and the benzodiazepine receptor agonist diazepam (3 mglkg) were investigated on spatial learning in the Morris water maze and thigmotaxia in an open field. Flu...

OBJECTIVE The diagnosis and management of mild traumatic brain injury continues to be a subject of debate, with varying opinions regarding the extent to which organically based impairments vs the impact of other stressors cause ongoing disability. The aim of this study was to elucidate the possible abnormalities in benzodiazepine receptor uptake in the brains of patients with mild traumatic bra...

Plasmodium falciparum relies on anion channels activated in the erythrocyte membrane to ensure the transport of nutrients and waste products necessary for its replication and survival after invasion. The molecular identity of these anion channels, termed "new permeability pathways" is unknown, but their currents correspond to up-regulation of endogenous channels displaying complex gating and ki...

Previous studies have demonstrated that gastric mucosa contained high levels of the polypeptide diazepam binding inhibitor, the endogenous ligand of the peripheral-type benzodiazepine receptor (PBR). However, the expression and function of this receptor protein in these tissues have not been investigated. Immunohistochemistry identified an intense PBR immunoreactivity in the mucous and parietal...

Binding levels of [3H]Ro5-4864, a ligand selective for peripheral-type benzodiazepine receptors, are substantially higher in homogenates of the olfactory bulb than in the rest of the brain. Among peripheral tissues evaluated, high levels of [3H]Ro5-4864 binding are found in the nasal epithelium. Drug displacement studies show that these binding sites are pharmacologically of the peripheral type...