Lorediplon is a nonbenzodiazepine of the pyrazolopyrimidine family that is being pursued as a treatment for insomnia but has not completed development. Lorediplon demonstrated a dose-dependent improvement in sleep, whereas zolpidem showed a more sustained WASO effect. No next-day hangover effects were observed. These sleep effects are also consistent with the pharmacokinetic profile of lorediplon. These results warrant clinical trials in patients with insomnia.
Chemical Formula: C20H15FN4O2S
Exact Mass: 394.08997
Molecular Weight: 394.42
Elemental Analysis: C, 60.90; H, 3.83; F, 4.82; N, 14.21; O, 8.11; S, 8.13
Chemical Name: N-[2-fluoro-5-[3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methylacetamide
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Zisapel N. Current Phase II investigational therapies for insomnia. Expert Opin Investig Drugs. 2015 Mar;24(3):401-11. doi: 10.1517/13543784.2015.987340. Epub 2014 Nov 25. Review. PubMed PMID: 25423562.
Horoszok L, Baleeiro T, D'Aniello F, Gropper S, Santos B, Guglietta A, Roth T. 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):266-73. doi: 10.1002/hup.2395. PubMed PMID: 24911577.
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