Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 20 of 34

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.

Inhibition of Orexin Signaling Promotes Sleep Yet Preserves Salient Arousability in Monkeys.

Tannenbaum PL, Tye SJ, Stevens J, Gotter AL, Fox SV, Savitz AT, Coleman PJ, Uslaner JM, Kuduk SD, Hargreaves R, Winrow CJ, Renger JJ.

Sleep. 2016 Mar 1;39(3):603-12. doi: 10.5665/sleep.5536.

4.

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
5.

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):4992-4999. doi: 10.1016/j.bmcl.2014.12.081. Epub 2015 Jan 6.

PMID:
25613676
6.

Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.

Raheem IT, Breslin MJ, Bruno J, Cabalu TD, Cooke A, Cox CD, Cui D, Garson S, Gotter AL, Fox SV, Harrell CM, Kuduk SD, Lemaire W, Prueksaritanont T, Renger JJ, Stump C, Tannenbaum PL, Williams PD, Winrow CJ, Coleman PJ.

Bioorg Med Chem Lett. 2015 Feb 1;25(3):444-50. doi: 10.1016/j.bmcl.2014.12.056. Epub 2014 Dec 23.

PMID:
25577040
7.

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
8.

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.

9.

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.

10.

Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant.

Kuduk SD, Skudlarek JW, Di Marco CN, Bruno JG, Pausch MA, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Gotter AL, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2014 Apr 1;24(7):1784-9. doi: 10.1016/j.bmcl.2014.02.026. Epub 2014 Feb 19.

PMID:
24630562
11.

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.

12.

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
13.

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.

14.

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.

15.

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.

16.

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
17.

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
18.

Discovery of a pharmacologically active antagonist of the two-pore-domain potassium channel K2P9.1 (TASK-3).

Coburn CA, Luo Y, Cui M, Wang J, Soll R, Dong J, Hu B, Lyon MA, Santarelli VP, Kraus RL, Gregan Y, Wang Y, Fox SV, Binns J, Doran SM, Reiss DR, Tannenbaum PL, Gotter AL, Meinke PT, Renger JJ.

ChemMedChem. 2012 Jan 2;7(1):123-33. doi: 10.1002/cmdc.201100351. Epub 2011 Sep 14.

PMID:
21916012
19.

TASK-3 as a potential antidepressant target.

Gotter AL, Santarelli VP, Doran SM, Tannenbaum PL, Kraus RL, Rosahl TW, Meziane H, Montial M, Reiss DR, Wessner K, McCampbell A, Stevens J, Brunner JI, Fox SV, Uebele VN, Bayliss DA, Winrow CJ, Renger JJ.

Brain Res. 2011 Oct 6;1416:69-79. doi: 10.1016/j.brainres.2011.08.021. Epub 2011 Aug 16.

20.

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. Erratum in: J Neurogenet. 2016 Sep - Dec;30(3-4):316.

PMID:
21473737

Supplemental Content

Loading ...
Support Center