Suvorexant (MK-4305) is an orexin receptor antagonist in development by Merck & Co.[1][2][3] This drug for sleep disorders has passed Phase II trials, and is one of several such compounds currently in development, the others being Actelion's ACT-078573 and GlaxoSmithKline's SB-649,868.
[edit] References
- ^ Christopher D. Cox, Michael J. Breslin, David B. Whitman, John D. Schreier, Georgia B. McGaughey, Michael J. Bogusky, Anthony J. Roecker, Swati P. Mercer, Rodney A. Bednar, Wei Lemaire, Joseph G. Bruno, Duane R. Reiss, C. Meacham Harrell, Kathy L. Murphy, Susan L. Garson, Scott M. Doran, Thomayant Prueksaritanont, Wayne B. Anderson, Cuyue Tang, Shane Roller, Tamara D. Cabalu, Donghui Cui, George D. Hartman, Steven D. Young, Ken S. Koblan, Christopher J. Winrow, John J. Renger and Paul J. Coleman. (2010). "Discovery of the Dual Orexin Receptor Antagonist [(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia.". Journal of Medicinal Chemistry 53 (14): 5320-5332. doi:10.1021/jm100541c. edit
- ^ Carl A. Baxter, Ed Cleator, Karel M. J. Brands, John S. Edwards, Robert A. Reamer, Faye J. Sheen, Gavin W. Stewart, Neil A. Strotman, and Debra J. Wallace. (2011). "The First Large-Scale Synthesis of MK-4305: A Dual Orexin Receptor Antagonist for the Treatment of Sleep Disorder.". Organic Process Research and Development 15 (2): 367-375. doi:10.1021.2Fop1002853. edit
- ^ Christopher J. Winrow, Anthony L. Gotter, Christopher D. Cox, Scott M. Doran, Pamela L. Tannenbaum, Michael J. Breslin, Susan L. Garson, Steven V. Fox, Charles M. Harrell, Joanne Stevens, Duane R. Reiss, Donghui Cui, Paul J. Coleman and John J. Renger. (2011). "Promotion of Sleep by Suvorexant—A Novel Dual Orexin Receptor Antagonist.". Journal of Neurogenetics 25 (1-2): 52-61. doi:10.3109.2F01677063.2011.566953. edit
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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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| α2-Adrenergic agonists |
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| 5-HT2A antagonists |
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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| Melatonin agonists |
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| Orexin antagonists |
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| Others |
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| Cholecystokinin |
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| CRH |
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| Galanin |
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| Ghrelin |
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| MCH |
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| Melanocortin |
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| Neuropeptide S |
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| Neuropeptide Y |
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| Neurotensin |
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| Opioid |
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| Orexin |
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| Oxytocin |
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| Tachykinin |
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Agonists: Substance P
Antagonists: Aprepitant • Befetupitant • Casopitant • CI-1021 • CP-96,345 • CP-99,994 • CP-122,721 • Dapitant • Ezlopitant • FK-888 • Fosaprepitant • GR-203,040 • GW-597,599 • HSP-117 • L-733,060 • L-741,671 • L-743,310 • L-758,298 • Lanepitant • LY-306,740 • Maropitant • Netupitant • NKP-608 • Nolpitantium • Orvepitant • RP-67,580 • SDZ NKT 343 • Vestipitant • Vofopitant
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| Vasopressin |
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