For research use only. Not for therapeutic Use.
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]
| Catalog Number | I005469 |
| CAS Number | 917393-39-6 |
| Synonyms | N-[2-fluoro-5-[3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methylacetamide |
| Molecular Formula | C20H15FN4O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C20H15FN4O2S/c1-12(26)24(2)17-10-13(5-6-15(17)21)16-7-8-22-20-14(11-23-25(16)20)19(27)18-4-3-9-28-18/h3-11H,1-2H3 |
| InChIKey | NQPOCLFSADOXBR-UHFFFAOYSA-N |
| SMILES | CC(=O)N(C)C1=C(C=CC(=C1)C2=CC=NC3=C(C=NN23)C(=O)C4=CC=CS4)F |
| Reference | [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. |
