SB-649,868
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SB649868)
SB-649,868 is an orexin receptor antagonist in development by GlaxoSmithKline.[1][2] Currently in Phase 2 development, this drug for sleep disorders is one of two such compounds currently in development, the other being Actelion's ACT-078573.
[edit] References
- ^ Renzulli C, Nash M, Wright M, Thomas S, Zamuner S, Pellegatti M, Bettica P, Boyle G (February 2011). "Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans". Drug Metabolism and Disposition: the Biological Fate of Chemicals 39 (2): 215–27. doi:10.1124/dmd.110.035386. PMID 21045199.
- ^ Bettica P, Nucci G, Pyke C, Squassante L, Zamuner S, Ratti E, Gomeni R, Alexander R (July 2011). "Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist". Journal of Psychopharmacology (Oxford, England). doi:10.1177/0269881111408954. PMID 21730017.
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| GABAA agonists/PAMs |
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| GABAB agonists |
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| H1 inverse agonists |
Antihistamines: Captodiame • Cyproheptadine • Diphenhydramine • Doxylamine • Hydroxyzine • Methapyrilene • Pheniramine • Promethazine • Propiomazine
Antidepressants: Tricyclic antidepressants ( Amitriptyline, Doxepin, Trimipramine, etc.) • Tetracyclic antidepressants ( Mianserin, Mirtazapine, etc.)
Antipsychotics: Typical antipsychotics ( Chlorpromazine, Thioridazine, etc.) • Atypical antipsychotics ( Olanzapine, Quetiapine, Risperidone, etc.)
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| α1-Adrenergic antagonists |
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Antidepressants: Serotonin antagonists and reuptake inhibitors ( Trazodone) • Tricyclic antidepressants ( Amitriptyline, Doxepin, Trimipramine, etc.) • Tetracyclic antidepressants ( Mianserin, Mirtazapine, etc.)
Antipsychotics: Typical antipsychotics ( Chlorpromazine, Thioridazine, etc.) • Atypical antipsychotics ( Olanzapine, Quetiapine, Risperidone, etc.)
Others: Eplivanserin • Niaprazine • Pruvanserin • Volinanserin
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| Orexin antagonists |
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| Cholecystokinin |
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| Orexin |
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- Agonists: Substance P
Antagonists: Aprepitant
- Befetupitant
- Casopitant
- CI-1021
- CP-96,345
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- L-743,310
- L-758,298
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- Vestipitant
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