Loreclezole was found to be active in all animal models of seizures, whether a genetic model of reflex epilepsy was used or models where seizures were elicited by chemical or electrical stimulation. In addition, loreclezole was active against both TON and CLON seizures and increased the threshold for behavioral as well as EEG seizures. Loreclezole has a very rapid onset of action and a duration of the activity, which in certain tests last for more than 24 hr. Chronic administration for 5-7 days did not lead to tolerance to the anticonvulsant action of loreclezole. Loreclezole potentiates gamma-aminobutyric acid (GABA) type A receptor function, by interacting with a specific allosteric modulatory site on receptor beta-subunits. It also acts as a negative modulator at a novel regulatory site, enhancing GABAA receptor sensitization. Inhibits homomeric ρ1 GABAC receptors.