Lorediplon is a novel hypnotic drug acting as a GABAA receptor modulator, differentially active at the α1-subunit, associated with promoting sleep.

In vivo, Lorediplon inhibits spontaneous motor activity and increases the duration of sleep in mice (ED50s = 0.13 and 1.2 mg/kg, respectively). It selectively inhibits spontaneous motor activity, which is driven by α1 subunit-containing GABAA receptors, over modification of muscular tone in mice, an α2 subunit-containing GABAA receptor-stimulated activity [1]. Lorediplon (0.13 and 1.2 mg/kg) also decreases latency to slow-wave sleep (SWS) and paradoxical sleep (PS) in mice [2].