917393-39-6 Usage
Description
Lorediplon is a non-benzodiazepine pyrazolopyrimidine compound under development for the management of insomnia. It acts as a GABAA receptor modulator, with a long plasma half-life that contributes to its hypnotic effect. Lorediplon has the potential to maintain sleep and preserve sleep architecture, showing better efficacy in quality and maintenance of sleep compared to zolpidem. It has been well-tolerated and safe with no residual effects compared to other sedative-hypnotics. Currently, Lorediplon has completed Phase II clinical trials, demonstrating strong efficacy in sleep maintenance and an acceptable safety profile.
Uses
Used in Pharmaceutical Industry:
Lorediplon is used as a GABAA receptor modulator for the treatment of insomnia. Its long plasma half-life and potential to maintain sleep and sleep architecture make it a promising candidate for managing sleep disorders. In clinical trials, it has shown strong efficacy in sleep maintenance and an acceptable safety profile, making it a potential alternative to traditional sedative-hypnotics.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 917393-39-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,1,7,3,9 and 3 respectively; the second part has 2 digits, 3 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 917393-39:
(8*9)+(7*1)+(6*7)+(5*3)+(4*9)+(3*3)+(2*3)+(1*9)=196
196 % 10 = 6
So 917393-39-6 is a valid CAS Registry Number.
917393-39-6Relevant articles and documents
PROCESS FOR THE PREPARATION OF N-[5-(3-DIMETHYLAMINO-ACRYLOYL)-2-FLUORO-PHENYL]-N-METHYL-ACETAMIDE
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Page/Page column 5, (2011/11/13)
The present invention relates to a new process for the preparation of N-[5-(3-dimethylamino-acryloyl)-2-fluorophenyl]-N-methyl-acetamide (I) in a high yield and high purity, which is an intermediate in the synthesis of compounds with affinity for GABAsub
PROCESS FOR THE MANUFACTURE OF A CRYSTALLINE PYRAZOLO[1,5-A]PYRIMIDINE COMPOUND
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Page/Page column 5-6, (2008/06/13)
The present invention relates to a novel process for the industrial manufacture of polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)- pyrazolo[1,5-a] pyrimidin-7-yl]-phenyl}-N-methyl-acetamide.
