Lorediplon

Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep. Target: GABA Lorediplon is a drug for the treatment of insomnia, has been successfully completed with a best-in-class efficacy profile in terms of maintaining sleep and sleep quality, Lorediplon targets GABAA. [1] Lorediplon demonstrates a minimum of 10-fold and 6-fold increase in potency (respectively) in the spontaneous motor activation studies. At concentrations of 1.2mg/kg, Lorediplon demonstrates a 57%increased effect on Slow Wave Sleep (SWS), when compared with a placebo.[2]

Product Specifications

CAS Number

[917393-39-6]

UNSPSC

12352005

Target

GABA Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Lorediplon.html

Purity

99.88

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC(N(C1=CC(C2=CC=NC3=C(C(C4=CC=CS4)=O)C=NN23)=CC=C1F)C)=O

Molecular Formula

C20H15FN4O2S

Molecular Weight

394.42

References & Citations

[1]Zisapel N. Current Phase II investigational therapies for insomnia. Expert Opin Investig Drugs. 2015 Mar;24 (3) :401-411.|[2]Horoszok L, et al. A single-dose, randomized, double-blind, double dummy, placebo and positive-controlled, five-way cross-over study to assess the pharmacodynamic effects of lorediplon in a phase advance model of insomnia in healthy Caucasian adult male subjects. Hum Psychopharmacol. 2014 May;29 (3) :266-273.