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Items: 1 to 20 of 131

1.

Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia.

Winrow CJ, Gotter AL, Cox CD, Tannenbaum PL, Garson SL, Doran SM, Breslin MJ, Schreier JD, Fox SV, Harrell CM, Stevens J, Reiss DR, Cui D, Coleman PJ, Renger JJ.

Neuropharmacology. 2012 Feb;62(2):978-87. doi: 10.1016/j.neuropharm.2011.10.003. Epub 2011 Oct 18.

PMID:
22019562
2.

Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties.

Coleman PJ, Schreier JD, Cox CD, Breslin MJ, Whitman DB, Bogusky MJ, McGaughey GB, Bednar RA, Lemaire W, Doran SM, Fox SV, Garson SL, Gotter AL, Harrell CM, Reiss DR, Cabalu TD, Cui D, Prueksaritanont T, Stevens J, Tannenbaum PL, Ball RG, Stellabott J, Young SD, Hartman GD, Winrow CJ, Renger JJ.

ChemMedChem. 2012 Mar 5;7(3):415-24, 337. doi: 10.1002/cmdc.201200025. Epub 2012 Feb 3.

PMID:
22307992
3.

Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist.

Winrow CJ, Gotter AL, Cox CD, Doran SM, Tannenbaum PL, Breslin MJ, Garson SL, Fox SV, Harrell CM, Stevens J, Reiss DR, Cui D, Coleman PJ, Renger JJ.

J Neurogenet. 2011 Mar;25(1-2):52-61. doi: 10.3109/01677063.2011.566953. Epub 2011 Apr 8.

PMID:
21473737
4.

The dual orexin receptor antagonist almorexant induces sleep and decreases orexin-induced locomotion by blocking orexin 2 receptors.

Mang GM, Dürst T, Bürki H, Imobersteg S, Abramowski D, Schuepbach E, Hoyer D, Fendt M, Gee CE.

Sleep. 2012 Dec 1;35(12):1625-35. doi: 10.5665/sleep.2232.

5.

Orexin in sleep, addiction and more: is the perfect insomnia drug at hand?

Hoyer D, Jacobson LH.

Neuropeptides. 2013 Dec;47(6):477-88. doi: 10.1016/j.npep.2013.10.009. Epub 2013 Oct 23. Review.

PMID:
24215799
6.

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.

Cox CD, Breslin MJ, Whitman DB, Schreier JD, McGaughey GB, Bogusky MJ, Roecker AJ, Mercer SP, Bednar RA, Lemaire W, Bruno JG, Reiss DR, Harrell CM, Murphy KL, Garson SL, Doran SM, Prueksaritanont T, Anderson WB, Tang C, Roller S, Cabalu TD, Cui D, Hartman GD, Young SD, Koblan KS, Winrow CJ, Renger JJ, Coleman PJ.

J Med Chem. 2010 Jul 22;53(14):5320-32. doi: 10.1021/jm100541c.

PMID:
20565075
7.

Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.

Di Fabio R, Pellacani A, Faedo S, Roth A, Piccoli L, Gerrard P, Porter RA, Johnson CN, Thewlis K, Donati D, Stasi L, Spada S, Stemp G, Nash D, Branch C, Kindon L, Massagrande M, Poffe A, Braggio S, Chiarparin E, Marchioro C, Ratti E, Corsi M.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. doi: 10.1016/j.bmcl.2011.06.086. Epub 2011 Jun 30.

PMID:
21831639
8.

Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptor antagonists.

Faedo S, Perdonà E, Antolini M, di Fabio R, Merlo Pich E, Corsi M.

Eur J Pharmacol. 2012 Oct 5;692(1-3):1-9. doi: 10.1016/j.ejphar.2012.07.007. Epub 2012 Jul 13.

PMID:
22796453
9.

Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor.

Malherbe P, Borroni E, Gobbi L, Knust H, Nettekoven M, Pinard E, Roche O, Rogers-Evans M, Wettstein JG, Moreau JL.

Br J Pharmacol. 2009 Apr;156(8):1326-41. doi: 10.1111/j.1476-5381.2009.00127.x.

10.

Orexin receptor subtype activation and locomotor behaviour in the rat.

Samson WK, Bagley SL, Ferguson AV, White MM.

Acta Physiol (Oxf). 2010 Mar;198(3):313-24. doi: 10.1111/j.1748-1716.2009.02056.x. Epub 2009 Nov 4.

11.

Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats.

Whitman DB, Cox CD, Breslin MJ, Brashear KM, Schreier JD, Bogusky MJ, Bednar RA, Lemaire W, Bruno JG, Hartman GD, Reiss DR, Harrell CM, Kraus RL, Li Y, Garson SL, Doran SM, Prueksaritanont T, Li C, Winrow CJ, Koblan KS, Renger JJ, Coleman PJ.

ChemMedChem. 2009 Jul;4(7):1069-74. doi: 10.1002/cmdc.200900069.

PMID:
19418500
12.

Orexin receptors: pharmacology and therapeutic opportunities.

Scammell TE, Winrow CJ.

Annu Rev Pharmacol Toxicol. 2011;51:243-66. doi: 10.1146/annurev-pharmtox-010510-100528. Review.

13.

Identification of MK-8133: An orexin-2 selective receptor antagonist with favorable development properties.

Kuduk SD, Skudlarek JW, DiMarco CN, Bruno JG, Pausch MH, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Garson SL, Savitz AT, Harrell CM, Gotter AL, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2015 Jun 15;25(12):2488-92. doi: 10.1016/j.bmcl.2015.04.066. Epub 2015 Apr 29.

PMID:
25981685
14.

International Union of Basic and Clinical Pharmacology. LXXXVI. Orexin receptor function, nomenclature and pharmacology.

Gotter AL, Webber AL, Coleman PJ, Renger JJ, Winrow CJ.

Pharmacol Rev. 2012 Jul;64(3):389-420. doi: 10.1124/pr.111.005546. Review.

15.

Role of orexin-1 receptor mechanisms on compulsive food consumption in a model of binge eating in female rats.

Piccoli L, Micioni Di Bonaventura MV, Cifani C, Costantini VJ, Massagrande M, Montanari D, Martinelli P, Antolini M, Ciccocioppo R, Massi M, Merlo-Pich E, Di Fabio R, Corsi M.

Neuropsychopharmacology. 2012 Aug;37(9):1999-2011. doi: 10.1038/npp.2012.48. Epub 2012 May 9.

16.

Differential roles of orexin receptor-1 and -2 in the regulation of non-REM and REM sleep.

Mieda M, Hasegawa E, Kisanuki YY, Sinton CM, Yanagisawa M, Sakurai T.

J Neurosci. 2011 Apr 27;31(17):6518-26. doi: 10.1523/JNEUROSCI.6506-10.2011.

17.

Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.

Roecker AJ, Mercer SP, Schreier JD, Cox CD, Fraley ME, Steen JT, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, Stevens J, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Stellabott J, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ.

ChemMedChem. 2014 Feb;9(2):311-22. doi: 10.1002/cmdc.201300447. Epub 2013 Dec 27.

PMID:
24376006
18.

Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.

Malherbe P, Borroni E, Pinard E, Wettstein JG, Knoflach F.

Mol Pharmacol. 2009 Sep;76(3):618-31. doi: 10.1124/mol.109.055152. Epub 2009 Jun 19.

19.

Orexin receptor antagonists differ from standard sleep drugs by promoting sleep at doses that do not disrupt cognition.

Uslaner JM, Tye SJ, Eddins DM, Wang X, Fox SV, Savitz AT, Binns J, Cannon CE, Garson SL, Yao L, Hodgson R, Stevens J, Bowlby MR, Tannenbaum PL, Brunner J, Mcdonald TP, Gotter AL, Kuduk SD, Coleman PJ, Winrow CJ, Renger JJ.

Sci Transl Med. 2013 Apr 3;5(179):179ra44. doi: 10.1126/scitranslmed.3005213.

20.

Orexin receptor antagonists: medicinal chemistry and therapeutic potential.

Roecker AJ, Coleman PJ.

Curr Top Med Chem. 2008;8(11):977-87. Review.

PMID:
18673167
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