A ligand for α1 subunit-containing GABAA receptors
Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.Target: GABALorediplon 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]
参考文献:
[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 s
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