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Page 1
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. Coburn CA, et al. Among authors: tannenbaum pl. ChemMedChem. 2012 Jan 2;7(1):123-33. doi: 10.1002/cmdc.201100351. Epub 2011 Sep 14. ChemMedChem. 2012. PMID: 21916012
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. Gotter AL, et al. Among authors: tannenbaum pl. Brain Res. 2011 Oct 6;1416:69-79. doi: 10.1016/j.brainres.2011.08.021. Epub 2011 Aug 16. Brain Res. 2011. PMID: 21885038 Free PMC article.
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. Coleman PJ, et al. Among authors: tannenbaum pl. ChemMedChem. 2012 Mar 5;7(3):415-24, 337. doi: 10.1002/cmdc.201200025. Epub 2012 Feb 3. ChemMedChem. 2012. PMID: 22307992
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. Roecker AJ, et al. Among authors: tannenbaum pl. ChemMedChem. 2014 Feb;9(2):311-22. doi: 10.1002/cmdc.201300447. Epub 2013 Dec 27. ChemMedChem. 2014. PMID: 24376006
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. Winrow CJ, et al. Among authors: tannenbaum pl. J Neurogenet. 2011 Mar;25(1-2):52-61. doi: 10.3109/01677063.2011.566953. Epub 2011 Apr 8. J Neurogenet. 2011. PMID: 21473737
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. Winrow CJ, et al. Among authors: tannenbaum pl. Neuropharmacology. 2012 Feb;62(2):978-87. doi: 10.1016/j.neuropharm.2011.10.003. Epub 2011 Oct 18. Neuropharmacology. 2012. PMID: 22019562
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. Uslaner JM, et al. Among authors: tannenbaum pl. Sci Transl Med. 2013 Apr 3;5(179):179ra44. doi: 10.1126/scitranslmed.3005213. Sci Transl Med. 2013. PMID: 23552372
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. Fox SV, et al. Among authors: tannenbaum pl. Neuropsychopharmacology. 2013 Nov;38(12):2401-8. doi: 10.1038/npp.2013.139. Epub 2013 May 31. Neuropsychopharmacology. 2013. PMID: 23722242 Free PMC article.
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. Gotter AL, et al. Among authors: tannenbaum pl. BMC Neurosci. 2013 Aug 28;14:90. doi: 10.1186/1471-2202-14-90. BMC Neurosci. 2013. PMID: 23981345 Free PMC article.
44 results