Lorediplon

Lorediplon is a ligand for α₁ subunit-containing GABA_A receptors.¹ In vivo, lorediplon inhibits spontaneous motor activity and increases 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 GABA_A receptors, over modification of muscular tone in mice, an α₂ subunit-containing GABA_A receptor-stimulated activity.² Lorediplon (0.13 and 1.2 mg/kg) also decreases latency to slow wave sleep (SWS) and paradoxical sleep (PS) in mice.³ Formulations containing lorediplon have been used in the treatment of insomnia.

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1. Stienen, P., Pérez, C., Alcántara, A.M., et al. In vivo pharmacological profile of GF-015535-00, a novel nonbenzodiazepine sedative-hypnotic. Society for Neuroscience (2009).

2. Stienen, P., Pérez, C., Alcántara, A., et al. CNS pharmacology of a novel non-benzodiazepine hypnotic, GF-015535-00, for the treatment of insomnia. Society of neuroscience (2010).

3. Anaclet, C., Zhang, M., Zhao, C., et al. Effects of GF-015535-00, a novel α1 GABA_A receptor ligand, on the sleep-wake cycle in mice, with reference to zolpidem. Sleep 35(1), 103-111 (2012).