Loreclezole

Loreclezole is a sedative and an anticonvulsant which acts as a GABAA receptor positive allosteric modulator.

[1] The binding site of loreclezole has been shown experimentally to be shared by valerenic acid, an extract of the root of the valerian plant.

[3] In addition, at low, nontoxic doses, the drug has anti-absence activity in a genetic model of generalized absence epilepsy.

Using native rat and cloned human GABA-A receptors, loreclezole strongly potentiated GABA-activated chloride current.

However, the activity of the drug did not require the presence of the γ-subunit and was not blocked by flumazenil, confirming that loreclezole does not interact with the benzodiazepine recognition site.