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Items: 1 to 20 of 27

1.

Investigation of orexin-2 selective receptor antagonists: Structural modifications resulting in dual orexin receptor antagonists.

Skudlarek JW, DiMarco CN, Babaoglu K, Roecker AJ, Bruno JG, Pausch MA, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Wuelfing WP, Garson SL, Fox SV, Savitz AT, Harrell CM, Gotter AL, Winrow CJ, Renger JJ, Kuduk SD, Coleman PJ.

Bioorg Med Chem Lett. 2017 Mar 15;27(6):1364-1370. doi: 10.1016/j.bmcl.2017.02.012. Epub 2017 Feb 9.

PMID:
28216403
2.

Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man.

Gotter AL, Forman MS, Harrell CM, Stevens J, Svetnik V, Yee KL, Li X, Roecker AJ, Fox SV, Tannenbaum PL, Garson SL, Lepeleire ID, Calder N, Rosen L, Struyk A, Coleman PJ, Herring WJ, Renger JJ, Winrow CJ.

Sci Rep. 2016 Jun 3;6:27147. doi: 10.1038/srep27147.

3.

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
4.

Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements.

Roecker AJ, Mercer SP, Bergman JM, Gilbert KF, Kuduk SD, Harrell CM, Garson SL, Fox SV, Gotter AL, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Lemaire W, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4992-9. doi: 10.1016/j.bmcl.2014.12.081. Epub 2015 Jan 6.

PMID:
25613676
5.

Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.

Roecker AJ, Reger TS, Mattern MC, Mercer SP, Bergman JM, Schreier JD, Cube RV, Cox CD, Li D, 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.

Bioorg Med Chem Lett. 2014 Oct 15;24(20):4884-90. doi: 10.1016/j.bmcl.2014.08.041. Epub 2014 Aug 26.

PMID:
25248679
6.

Differential sleep-promoting effects of dual orexin receptor antagonists and GABAA receptor modulators.

Gotter AL, Garson SL, Stevens J, Munden RL, Fox SV, Tannenbaum PL, Yao L, Kuduk SD, McDonald T, Uslaner JM, Tye SJ, Coleman PJ, Winrow CJ, Renger JJ.

BMC Neurosci. 2014 Sep 22;15:109. doi: 10.1186/1471-2202-15-109.

7.

Orexin receptor antagonist-induced sleep does not impair the ability to wake in response to emotionally salient acoustic stimuli in dogs.

Tannenbaum PL, Stevens J, Binns J, Savitz AT, Garson SL, Fox SV, Coleman P, Kuduk SD, Gotter AL, Marino M, Tye SJ, Uslaner JM, Winrow CJ, Renger JJ.

Front Behav Neurosci. 2014 May 16;8:182. doi: 10.3389/fnbeh.2014.00182. eCollection 2014.

8.

Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.

Roecker AJ, Mercer SP, Harrell CM, Garson SL, Fox SV, Gotter AL, Prueksaritanont T, Cabalu TD, Cui D, Lemaire W, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2014 May 1;24(9):2079-85. doi: 10.1016/j.bmcl.2014.03.052. Epub 2014 Mar 26.

PMID:
24704030
9.

Dual orexin receptor antagonists show distinct effects on locomotor performance, ethanol interaction and sleep architecture relative to gamma-aminobutyric acid-A receptor modulators.

Ramirez AD, Gotter AL, Fox SV, Tannenbaum PL, Yao L, Tye SJ, McDonald T, Brunner J, Garson SL, Reiss DR, Kuduk SD, Coleman PJ, Uslaner JM, Hodgson R, Browne SE, Renger JJ, Winrow CJ.

Front Neurosci. 2013 Dec 24;7:254. doi: 10.3389/fnins.2013.00254. eCollection 2013.

10.

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
11.

The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold.

Gotter AL, Winrow CJ, Brunner J, Garson SL, Fox SV, Binns J, Harrell CM, Cui D, Yee KL, Stiteler M, Stevens J, Savitz A, Tannenbaum PL, Tye SJ, McDonald T, Yao L, Kuduk SD, Uslaner J, Coleman PJ, Renger JJ.

BMC Neurosci. 2013 Aug 28;14:90. doi: 10.1186/1471-2202-14-90.

12.

Quantitative electroencephalography within sleep/wake states differentiates GABAA modulators eszopiclone and zolpidem from dual orexin receptor antagonists in rats.

Fox SV, Gotter AL, Tye SJ, Garson SL, Savitz AT, Uslaner JM, Brunner JI, Tannenbaum PL, McDonald TP, Hodgson R, Yao L, Bowlby MR, Kuduk SD, Coleman PJ, Hargreaves R, Winrow CJ, Renger JJ.

Neuropsychopharmacology. 2013 Nov;38(12):2401-8. doi: 10.1038/npp.2013.139. Epub 2013 May 31.

13.

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.

14.

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
15.

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
16.

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
17.

Pyridyl amides as potent inhibitors of T-type calcium channels.

Reger TS, Yang ZQ, Schlegel KA, Shu Y, Mattern C, Cube R, Rittle KE, McGaughey GB, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Li Y, Kraus RL, Uebele VN, Renger JJ, Barrow JC.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1692-6. doi: 10.1016/j.bmcl.2011.01.089. Epub 2011 Jan 26.

PMID:
21316226
18.

Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents.

Yang ZQ, Schlegel KA, Shu Y, Reger TS, Cube R, Mattern C, Coleman PJ, Small J, Hartman GD, Ballard J, Tang C, Kuo Y, Prueksaritanont T, Nuss CE, Doran S, Fox SV, Garson SL, Li Y, Kraus RL, Uebele VN, Taylor AB, Zeng W, Fang W, Chavez-Eng C, Troyer MD, Luk JA, Laethem T, Cook WO, Renger JJ, Barrow JC.

ACS Med Chem Lett. 2010 Aug 24;1(9):504-9. doi: 10.1021/ml100170e. eCollection 2010 Dec 9.

19.

Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists.

Schlegel KA, Yang ZQ, Reger TS, Shu Y, Cube R, Rittle KE, Bondiskey P, Bock MG, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Kraus RL, Li Y, Uebele VN, Renger JJ, Barrow JC.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5147-52. doi: 10.1016/j.bmcl.2010.07.010. Epub 2010 Jul 8.

PMID:
20673719
20.

Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.

Coleman PJ, Schreier JD, Roecker AJ, Mercer SP, McGaughey GB, Cox CD, Hartman GD, Harrell CM, Reiss DR, Doran SM, Garson SL, Anderson WB, Tang C, Prueksaritanont T, Winrow CJ, Renger JJ.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4201-5. doi: 10.1016/j.bmcl.2010.05.047. Epub 2010 May 25.

PMID:
20610153

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