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Review

Antagonists of the orexin receptors

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Pages 631-646 | Published online: 25 Apr 2006

Keep up to date with the latest research on this topic with citation updates for this article.

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Octavian C Ioachimescu & Ali A El-Solh. (2012) Pharmacotherapy of insomnia. Expert Opinion on Pharmacotherapy 13:9, pages 1243-1260.
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Paul J Coleman & John J Renger. (2010) Orexin receptor antagonists: a review of promising compounds patented since 2006. Expert Opinion on Therapeutic Patents 20:3, pages 307-324.
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Seiji Nishino. (2007) The hypocretin/orexin receptor: therapeutic prospective in sleep disorders. Expert Opinion on Investigational Drugs 16:11, pages 1785-1797.
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Mathieu RappasAmmar A. E. AliKirstie A. BennettJason D. BrownSarah J. BucknellMiles Congreve, Robert M. CookeGabriella CsekeChris de GraafAndrew S. DoréJames C. ErreyAli JazayeriFiona H. MarshallJonathan S. MasonRichard MouldJayesh C. PatelBenjamin G. TehanMalcolm WeirJohn A. Christopher. (2019) Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis. Journal of Medicinal Chemistry 63:4, pages 1528-1543.
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Bibia Heidmann, John Gatfield, Catherine Roch, Alexander Treiber, Simone Tortoioli, Christine Brotschi, Jodi T. Williams, Martin H. Bolli, Stefan Abele, Thierry Sifferlen, François Jenck & Christoph Boss. (2016) Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach. ChemMedChem 11:19, pages 2132-2146.
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Terry P. Lebold, Pascal Bonaventure & Brock T. Shireman. (2013) Selective orexin receptor antagonists. Bioorganic & Medicinal Chemistry Letters 23:17, pages 4761-4769.
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Rong Jiang, Xinyi Song, Purva Bali, Anthony Smith, Claudia Ruiz Bayona, Li Lin, Michael D. Cameron, Patricia H. McDonald, Paul J. Kenny & Theodore M. Kamenecka. (2012) Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists. Bioorganic & Medicinal Chemistry Letters 22:12, pages 3890-3894.
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Thomas E. ScammellChristopher J. Winrow. (2011) Orexin Receptors: Pharmacology and Therapeutic Opportunities. Annual Review of Pharmacology and Toxicology 51:1, pages 243-266.
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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 & Paul J. Coleman. (2010) Discovery of the Dual Orexin Receptor Antagonist [(7 R )-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2 H -1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia . Journal of Medicinal Chemistry 53:14, pages 5320-5332.
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Akira Terao & Masaomi Miyamoto. (2007) Recent and potential drugs for treatment of insomnia. Folia Pharmacologica Japonica 129:1, pages 35-41.
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