Lorediplon

Modify Date: 2024-01-02 18:23:10

Lorediplon Structure
Lorediplon structure
Common Name Lorediplon
CAS Number 917393-39-6 Molecular Weight 394.42200
Density N/A Boiling Point N/A
Molecular Formula C20H15FN4O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Lorediplon


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]

 Names

Name N-[2-fluoro-5-[3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methylacetamide
Synonym More Synonyms

 Lorediplon Biological Activity

Description 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]
Related Catalog
References

[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

 Chemical & Physical Properties

Molecular Formula C20H15FN4O2S
Molecular Weight 394.42200
Exact Mass 394.09000
PSA 95.81000
LogP 3.81060

 Synonyms

Lorediplon
N-(2-Fluoro-5-(3-(thiophene-2-carbonyl)pyrazolo(1,5-a)pyrimidin-7-yl)phenyl)-N-methylacetamide
Lorediplon [INN]
Acetamide,N-(2-fluoro-5-(3-(2-thienylcarbonyl)pyrazolo(1,5-a)pyrimidin-7-yl)phenyl)-N-methyl
UNII-VKU6Z23NSY
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