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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.


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.


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.


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.


Effects of eszopiclone and zolpidem on sleep-wake behavior, anxiety-like behavior and contextual memory in rats.

Huang MP, Radadia K, Macone BW, Auerbach SH, Datta S.

Behav Brain Res. 2010 Jun 26;210(1):54-66. doi: 10.1016/j.bbr.2010.02.018. Epub 2010 Feb 12.


The impact of age on the hypnotic effects of eszopiclone and zolpidem in the guinea pig.

Xi M, Chase MH.

Psychopharmacology (Berl). 2009 Jul;205(1):107-17. doi: 10.1007/s00213-009-1520-9. Epub 2009 Apr 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.


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.


Differential effects of a dual orexin receptor antagonist (SB-649868) and zolpidem on sleep initiation and consolidation, SWS, REM sleep, and EEG power spectra in a model of situational insomnia.

Bettica P, Squassante L, Groeger JA, Gennery B, Winsky-Sommerer R, Dijk DJ.

Neuropsychopharmacology. 2012 Apr;37(5):1224-33. doi: 10.1038/npp.2011.310. Epub 2012 Jan 11.


The dual orexin receptor antagonist, DORA-22, lowers histamine levels in the lateral hypothalamus and prefrontal cortex without lowering hippocampal acetylcholine.

Yao LL, Ramirez A, Roecker AJ, Fox S, Uslaner J, Smith SM, Hodgson R, Coleman PJ, Renger JJ, Winrow CJ, Gotter AL.

J Neurochem. 2017 Apr 26. doi: 10.1111/jnc.14055. [Epub ahead of print]


Differential effects of the dual orexin receptor antagonist almorexant and the GABA(A)-α1 receptor modulator zolpidem, alone or combined with ethanol, on motor performance in the rat.

Steiner MA, Lecourt H, Strasser DS, Brisbare-Roch C, Jenck F.

Neuropsychopharmacology. 2011 Mar;36(4):848-56. doi: 10.1038/npp.2010.224. Epub 2010 Dec 8.


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.


The modulation of synaptic GABA(A) receptors in the thalamus by eszopiclone and zolpidem.

Jia F, Goldstein PA, Harrison NL.

J Pharmacol Exp Ther. 2009 Mar;328(3):1000-6. doi: 10.1124/jpet.108.146084. Epub 2008 Nov 25.


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.


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.


Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia.

Bonaventure P, Shelton J, Yun S, Nepomuceno D, Sutton S, Aluisio L, Fraser I, Lord B, Shoblock J, Welty N, Chaplan SR, Aguilar Z, Halter R, Ndifor A, Koudriakova T, Rizzolio M, Letavic M, Carruthers NI, Lovenberg T, Dugovic C.

J Pharmacol Exp Ther. 2015 Sep;354(3):471-82. doi: 10.1124/jpet.115.225466. Epub 2015 Jul 15.


The Discovery of Suvorexant, the First Orexin Receptor Drug for Insomnia.

Coleman PJ, Gotter AL, Herring WJ, Winrow CJ, Renger JJ.

Annu Rev Pharmacol Toxicol. 2017 Jan 6;57:509-533. doi: 10.1146/annurev-pharmtox-010716-104837.


Central nervous system sites of the sleep promoting effects of eszopiclone in rats.

Kumar S, Alam MN, Rai S, Bashir T, McGinty D, Szymusiak R.

Neuroscience. 2011 May 5;181:67-78. doi: 10.1016/j.neuroscience.2011.03.006. Epub 2011 Mar 5.


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