to obtain drugs which are more selective at benzodiazepine (bzd) receptors, design and synthesis of functionally selective ligands for bzd receptors is the current strategy of our pharmaceutical chemistry department. the affinity of newly synthesized ligands is assessed by radioligand receptor binding assays. based on our previous studies, 2-phenyl-5-oxo-7-methyl-1,3,4-oxadiazolo[a,2,3]-pyrimid...

Although GABAA receptors have long been implicated in mediating ethanol (EtOH) actions, receptors containing the ‘‘nonsynaptic’’ subunit only recently have been shown to be uniquely sensitive to EtOH. Here, we show that subunit-containing receptors bind the imidazo-benzodiazepines (BZs) flumazenil and Ro15-4513 with high affinity (Kd < 10 nM), contrary to the widely held belief that these recep...

We describe the care for an elderly woman who was admitted to the intensive care unit (ICU) to receive noninvasive ventilation for acute exacerbation of chronic obstructive pulmonary disease. After administration of the sleeping pill zopiclone, a nonbenzodiazepine receptor agonist (NBRA), the patient became agitated and was confused, a possible paradoxical reaction to benzodiazepines. These sym...

Interactions of mu-opioid receptors with the benzodiazepine system were studied by examining the modulatory effects of flumazenil (a benzodiazepine antagonist) and alprazolam (a benzodiazepine agonist) on the respiratory effects of the opioid peptide dermorphin. Dermorphin, 1-30 nmol administered i.c.v., to conscious, unrestrained rats decreased ventilation rate (VR) and minute volume (MV) dose...

Stupor is defined as a deep sleep or behaviourally similar unresponsiveness from which the subject can be aroused only by vigorous repeated stimuli. Causes of stupor may be related to brain damage, toxic or metabolic encephalopathies. Idiopathic recurring stupor is a stupurous condition of unknown aetiology, unrelated to structural, toxic or metabolic disturbance. This condition responds to flu...

The anticonvulsant activity of Astragalus squarrosus total extract was assessed in pentylenetetrazole (PTZ)-induced convulsion in mice, with diazepam as the standard drug, while mechanistic studies were also conducted using flumazenil, a GABA A-benzodiazepine receptor complex site antagonist. The extract produced protection against convulsion at 400 mg/kg, comparable with protection of...