Lorediplon Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMF: 25 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 14 mg/ml

form 

A crystalline solid

color 

Light yellow to yellow

Lorediplon Usage And Synthesis

Description

Lorediplon is a non-benzodiazepine belonging to pyrazolopyrimidine family isunderdevelopment for the management for insomnia. Lorediplon acts by modulationof the GABAgreceptor. Its long plasma half-life has the potential of hypnotic effect. Ithas the potential for maintenance of sleep and the sleep architecture. In the phase Ipharmacodynamic study,it showed better efficacy in quality and maintenance ofsleep as compared with zolpidem. It has been shown to be well tolerated, safe with noresidual effects as compared with other sedative-hypnotic. Currently, the drug has completed Phase ll clinical trial. Results indicated strongefficacy in sleep maintenance with an acceptable safety profile. It also seems topreserve natural sleep architecture.

Uses

Lorediplon is GABAA receptor modulator and is used in the treatment of insomnia.

Biological Activity

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

References

[1] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras.
[2] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras.
[3] CHRISTELLE ANACLET. Effects of GF-015535-00, a novel α1 GABA A receptor ligand, on the sleep-wake cycle in mice, with reference to zolpidem.[J]. Sleep, 2012, 35 1: 103-111. DOI: 10.5665/sleep.1596