Flurazepam and chlordiazepam also are anxiolytic. Benzodiazepines exhibit anxiolytic activity due to their ability to promote GABA binding. The act as indirect agonists. Several ligands can block the actions of benzodiazepines, including flumazenil, a benzodiazepine antagonist. Benzodiazepine antagonists have no action by themselves but prevent the enhancement of GABA activity by the benzodiazepines.
Benzodiazepines possess anticonvulsant activity in addition to their anxiolytic action.
Recent efforts have focused on the development of compounds that exhibit selectivity for different combinations of subunits. Zolpidem and alpidem discriminate between GABA A receptors with different subunit composition. These compounds also can differentiate between the anticonvulsant and anxiolytic actions of the benzodiazepines. Within the class of b -carbolines, molecules with varying potency and efficacy have been developed for benzodiazepine binding sites. They block the binding of benzodiazepines and act as inverse agonists since they produce the opposite effect of diazepam.