Chemistry:SB-649868
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Short description: Chemical compound
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| Formula | C26H24FN3O3S |
| Molar mass | 477.55 g·mol−1 |
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SB-649868 is a dual orexin receptor antagonist that was being developed by GlaxoSmithKline as a treatment for insomnia.[1]
A phase I clinical trial evaluated doses up to 80 mg, resulting in significant improvement in sleep latency without adverse effects.[2] In randomized, double-blind, placebo-controlled crossover trials, the 10 and 30 mg doses increased sleep time and reduced sleep latency.[3] The subsequent phase II study added a 60 mg dose and observed dose-dependent sleep promotion.[4]
The compound no longer appears to be under active development, with the last study posted to ClinicalTrials.gov completed in 2010.
See also
References
- ↑ "Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans". Drug Metabolism and Disposition 39 (2): 215–27. February 2011. doi:10.1124/dmd.110.035386. PMID 21045199.
- ↑ "Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist". Journal of Psychopharmacology 26 (8): 1058–70. August 2012. doi:10.1177/0269881111408954. PMID 21730017.
- ↑ "Differential effects of a dual orexin receptor antagonist (SB-649868) and zolpidem on sleep initiation and consolidation, SWS, REM sleep, and EEG power spectra in a model of situational insomnia". Neuropsychopharmacology 37 (5): 1224–33. April 2012. doi:10.1038/npp.2011.310. PMID 22237311.
- ↑ "The orexin antagonist SB-649868 promotes and maintains sleep in men with primary insomnia". Sleep 35 (8): 1097–104. August 2012. doi:10.5665/sleep.1996. PMID 22851805.
Further reading
- Ratti E (December 13, 2007). "Psychiatry: An Innovative Drug Discovery Pipeline". http://www.mudin.net/more-gsk-neurosciences-seminar-13-dec-2007-emiliangelo-ratti--253710.html.
- "Orexin receptors: pharmacology and therapeutic opportunities". Annual Review of Pharmacology and Toxicology 51: 243–66. February 2011. doi:10.1146/annurev-pharmtox-010510-100528. PMID 21034217.
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