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Items: 1 to 50 of 144

1.

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

Yao L, Ramirez AD, Roecker AJ, Fox SV, Uslaner JM, Smith SM, Hodgson R, Coleman PJ, Renger JJ, Winrow CJ, Gotter AL.

J Neurochem. 2017 Jul;142(2):204-214. doi: 10.1111/jnc.14055. Epub 2017 Jun 1.

2.

Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice.

Roecker AJ, Egbertson M, Jones KLG, Gomez R, Kraus RL, Li Y, Koser AJ, Urban MO, Klein R, Clements M, Panigel J, Daley C, Wang J, Finger EN, Majercak J, Santarelli V, Gregan I, Cato M, Filzen T, Jovanovska A, Wang YH, Wang D, Joyce LA, Sherer EC, Peng X, Wang X, Sun H, Coleman PJ, Houghton AK, Layton ME.

Bioorg Med Chem Lett. 2017 May 15;27(10):2087-2093. doi: 10.1016/j.bmcl.2017.03.085. Epub 2017 Mar 30.

PMID:
28389149
3.

Discovery and optimization of 2-pyridinone aminal integrase strand transfer inhibitors for the treatment of HIV.

Schreier JD, Embrey MW, Raheem IT, Barbe G, Campeau LC, Dubost D, McCabe Dunn J, Grobler J, Hartingh TJ, Hazuda DJ, Klein D, Miller MD, Moore KP, Nguyen N, Pajkovic N, Powell DA, Rada V, Sanders JM, Sisko J, Steele TG, Wai J, Walji A, Xu M, Coleman PJ.

Bioorg Med Chem Lett. 2017 May 1;27(9):2038-2046. doi: 10.1016/j.bmcl.2017.02.039. Epub 2017 Feb 20.

PMID:
28285916
4.

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
5.

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. Review.

PMID:
27860547
6.

Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology.

Stump CA, Cooke AJ, Bruno J, Cabalu TD, Gotter AL, Harell CM, Kuduk SD, McDonald TP, O'Brien J, Renger JJ, Williams PD, Winrow CJ, Coleman PJ.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5809-5814. doi: 10.1016/j.bmcl.2016.10.019. Epub 2016 Oct 14.

PMID:
27818110
7.

Pharmacological evaluation of orexin receptor antagonists in preclinical animal models of pain.

McDonald T, Liang HA, Sanoja R, Gotter AL, Kuduk SD, Coleman PJ, Smith KM, Winrow CJ, Renger JJ.

J Neurogenet. 2016 Mar;30(1):32-41. doi: 10.3109/01677063.2016.1171862.

PMID:
27276194
8.

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.

9.

Discovery of 6-(Fluoro-(18)F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine ([(18)F]-MK-6240): A Positron Emission Tomography (PET) Imaging Agent for Quantification of Neurofibrillary Tangles (NFTs).

Walji AM, Hostetler ED, Selnick H, Zeng Z, Miller P, Bennacef I, Salinas C, Connolly B, Gantert L, Holahan M, O'Malley S, Purcell M, Riffel K, Li J, Balsells J, OBrien JA, Melquist S, Soriano A, Zhang X, Ogawa A, Xu S, Joshi E, Della Rocca J, Hess FJ, Schachter J, Hesk D, Schenk D, Struyk A, Babaoglu K, Lohith TG, Wang Y, Yang K, Fu J, Evelhoch JL, Coleman PJ.

J Med Chem. 2016 May 26;59(10):4778-89. doi: 10.1021/acs.jmedchem.6b00166. Epub 2016 May 5.

PMID:
27088900
10.

Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors.

Yin J, Babaoglu K, Brautigam CA, Clark L, Shao Z, Scheuermann TH, Harrell CM, Gotter AL, Roecker AJ, Winrow CJ, Renger JJ, Coleman PJ, Rosenbaum DM.

Nat Struct Mol Biol. 2016 Apr;23(4):293-9. doi: 10.1038/nsmb.3183. Epub 2016 Mar 7.

PMID:
26950369
11.

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.

12.

Correction to Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors.

Raheem IT, Walji AM, Klein D, Sanders JM, Powell DA, Abeywickrema P, Barbe G, Bennet A, Childers K, Christensen M, Clas SD, Dubost D, Embrey M, Grobler J, Hafey MJ, Hartingh TJ, Hazuda DJ, Kuethe JT, McCabe Dunn J, Miller MD, Moore KP, Nolting A, Pajkovic N, Patel S, Peng Z, Rada V, Rearden P, Schreier JD, Sisko J, Steele TG, Truchon JF, Wai J, Xu M, Coleman PJ.

J Med Chem. 2016 Jan 14;59(1):486. doi: 10.1021/acs.jmedchem.5b01957. Epub 2015 Dec 28. No abstract available.

PMID:
26709958
13.

Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.

Raheem IT, Schreier JD, Fuerst J, Gantert L, Hostetler ED, Huszar S, Joshi A, Kandebo M, Kim SH, Li J, Ma B, McGaughey G, Sharma S, Shipe WD, Uslaner J, Vandeveer GH, Yan Y, Renger JJ, Smith SM, Coleman PJ, Cox CD.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):126-32. doi: 10.1016/j.bmcl.2015.11.013. Epub 2015 Nov 10.

PMID:
26602277
14.

Preclinical Characterization of the Phosphodiesterase 10A PET Tracer [(11)C]MK-8193.

Hostetler ED, Fan H, Joshi AD, Zeng Z, Eng W, Gantert L, Holahan M, Meng X, Miller P, O'Malley S, Purcell M, Riffel K, Salinas C, Williams M, Ma B, Buist N, Smith SM, Coleman PJ, Cox CD, Flores BA, Raheem IT, Cook JJ, Evelhoch JL.

Mol Imaging Biol. 2016 Aug;18(4):579-87. doi: 10.1007/s11307-015-0910-0.

PMID:
26596571
15.

Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors.

Raheem IT, Walji AM, Klein D, Sanders JM, Powell DA, Abeywickrema P, Barbe G, Bennet A, Childers K, Christensen M, Clas SD, Dubost D, Embrey M, Grobler J, Hafey MJ, Hartingh TJ, Hazuda DJ, Kuethe JT, McCabe Dunn J, Miller MD, Moore KP, Nolting A, Pajkovic N, Patel S, Peng Z, Rada V, Rearden P, Schreier JD, Sisko J, Steele TG, Truchon JF, Wai J, Xu M, Coleman PJ.

J Med Chem. 2015 Oct 22;58(20):8154-65. doi: 10.1021/acs.jmedchem.5b01037. Epub 2015 Oct 8. Erratum in: J Med Chem. 2016 Jan 14;59(1):486. Childers, Karla [added]; Christensen, Melodie [added]; Kuethe, Jeffrey T. [added]; McCabe Dunn, Jamie [added]; Nolting, Andrew [added]; Peng, Zuihui [corrected].

PMID:
26397965
16.

Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis.

Shipe WD, Sharik SS, Barrow JC, McGaughey GB, Theberge CR, Uslaner JM, Yan Y, Renger JJ, Smith SM, Coleman PJ, Cox CD.

J Med Chem. 2015 Oct 8;58(19):7888-94. doi: 10.1021/acs.jmedchem.5b00983. Epub 2015 Sep 25.

PMID:
26378882
17.

Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.

Roecker AJ, Cox CD, Coleman PJ.

J Med Chem. 2016 Jan 28;59(2):504-30. doi: 10.1021/acs.jmedchem.5b00832. Epub 2015 Sep 15. Review.

PMID:
26317591
18.

Discovery of [¹¹C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.

Cox CD, Hostetler ED, Flores BA, Evelhoch JL, Fan H, Gantert L, Holahan M, Eng W, Joshi A, McGaughey G, Meng X, Purcell M, Raheem IT, Riffel K, Yan Y, Renger JJ, Smith SM, Coleman PJ.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4893-4898. doi: 10.1016/j.bmcl.2015.05.080. Epub 2015 Jun 1.

PMID:
26077491
19.

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
20.

P2-quinazolinones and bis-macrocycles as new templates for next-generation hepatitis C virus NS3/4a protease inhibitors: discovery of MK-2748 and MK-6325.

Rudd MT, Butcher JW, Nguyen KT, McIntyre CJ, Romano JJ, Gilbert KF, Bush KJ, Liverton NJ, Holloway MK, Harper S, Ferrara M, DiFilippo M, Summa V, Swestock J, Fritzen J, Carroll SS, Burlein C, DiMuzio JM, Gates A, Graham DJ, Huang Q, McClain S, McHale C, Stahlhut MW, Black S, Chase R, Soriano A, Fandozzi CM, Taylor A, Trainor N, Olsen DB, Coleman PJ, Ludmerer SW, McCauley JA.

ChemMedChem. 2015 Apr;10(4):727-35. doi: 10.1002/cmdc.201402558. Epub 2015 Mar 10.

PMID:
25759009
21.

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
22.

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
23.

Discovery of MK-8970: an acetal carbonate prodrug of raltegravir with enhanced colonic absorption.

Walji AM, Sanchez RI, Clas SD, Nofsinger R, de Lera Ruiz M, Li J, Bennet A, John C, Bennett DJ, Sanders JM, Di Marco CN, Kim SH, Balsells J, Ceglia SS, Dang Q, Manser K, Nissley B, Wai JS, Hafey M, Wang J, Chessen G, Templeton A, Higgins J, Smith R, Wu Y, Grobler J, Coleman PJ.

ChemMedChem. 2015 Feb;10(2):245-52. doi: 10.1002/cmdc.201402393. Epub 2014 Dec 2.

PMID:
25469982
24.

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
25.

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.

26.

Novel Quinoline-Based P2-P4 Macrocyclic Derivatives As Pan-Genotypic HCV NS3/4a Protease Inhibitors.

Shah U, Jayne C, Chackalamannil S, Velázquez F, Guo Z, Buevich A, Howe JA, Chase R, Soriano A, Agrawal S, Rudd MT, McCauley JA, Liverton NJ, Romano J, Bush K, Coleman PJ, Grisé-Bard C, Brochu MC, Charron S, Aulakh V, Bachand B, Beaulieu P, Zaghdane H, Bhat S, Han Y, Vacca JP, Davies IW, Weber AE, Venkatraman S.

ACS Med Chem Lett. 2014 Jan 9;5(3):264-9. doi: 10.1021/ml400466p. eCollection 2014 Mar 13.

27.

Selective orexin 2 receptor antagonism blocks cue-induced reinstatement, but not nicotine self-administration or nicotine-induced reinstatement.

Uslaner JM, Winrow CJ, Gotter AL, Roecker AJ, Coleman PJ, Hutson PH, Le AD, Renger JJ.

Behav Brain Res. 2014 Aug 1;269:61-5. doi: 10.1016/j.bbr.2014.04.012. Epub 2014 Apr 18.

PMID:
24746488
28.

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
29.

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
30.

Quantitative proteomics in laser capture microdissected sleep nuclei from rat brain.

Miller RA, Winrow CJ, Spellman DS, Song Q, Reiss DR, Conway JP, Taylor RR, Coleman PJ, Hendrickson RC, Renger JJ.

J Neurogenet. 2014 Mar-Jun;28(1-2):136-45. doi: 10.3109/01677063.2014.883389. Epub 2014 Mar 3.

31.

Shaping suvorexant: application of experimental and theoretical methods for driving synthetic designs.

McGaughey G, Bayly CI, Cox CD, Schreier JD, Breslin MJ, Bogusky M, Pitzenberger S, Ball R, Coleman PJ.

J Comput Aided Mol Des. 2014 Jan;28(1):5-12. doi: 10.1007/s10822-014-9710-x. Epub 2014 Feb 1.

32.

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.

33.

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
34.

Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs).

Mercer SP, Roecker AJ, Garson S, Reiss DR, Meacham Harrell C, Murphy KL, Bruno JG, Bednar RA, Lemaire W, Cui D, Cabalu TD, Tang C, Prueksaritanont T, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6620-4. doi: 10.1016/j.bmcl.2013.10.045. Epub 2013 Oct 30.

PMID:
24215892
35.

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.

36.

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.

37.

Twenty years of measurement of polycyclic aromatic hydrocarbons (PAHs) in UK ambient air by nationwide air quality networks.

Brown AS, Brown RJ, Coleman PJ, Conolly C, Sweetman AJ, Jones KC, Butterfield DM, Sarantaridis D, Donovan BJ, Roberts I.

Environ Sci Process Impacts. 2013 Jun;15(6):1199-215. doi: 10.1039/c3em00126a. Review.

PMID:
23636622
38.

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.

39.

Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.

Raheem IT, Breslin MJ, Fandozzi C, Fuerst J, Hill N, Huszar S, Kandebo M, Kim SH, Ma B, McGaughey G, Renger JJ, Schreier JD, Sharma S, Smith S, Uslaner J, Yan Y, Coleman PJ, Cox CD.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5903-8. doi: 10.1016/j.bmcl.2012.07.072. Epub 2012 Jul 27.

PMID:
22892116
40.

Orexin receptors as therapeutic drug targets.

Gotter AL, Roecker AJ, Hargreaves R, Coleman PJ, Winrow CJ, Renger JJ.

Prog Brain Res. 2012;198:163-88. doi: 10.1016/B978-0-444-59489-1.00010-0. Review.

PMID:
22813974
41.

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.

42.

The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey.

Smith SM, Uslaner JM, Cox CD, Huszar SL, Cannon CE, Vardigan JD, Eddins D, Toolan DM, Kandebo M, Yao L, Raheem IT, Schreier JD, Breslin MJ, Coleman PJ, Renger JJ.

Neuropharmacology. 2013 Jan;64:215-23. doi: 10.1016/j.neuropharm.2012.06.013. Epub 2012 Jun 27.

PMID:
22750078
43.

MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants.

Summa V, Ludmerer SW, McCauley JA, Fandozzi C, Burlein C, Claudio G, Coleman PJ, Dimuzio JM, Ferrara M, Di Filippo M, Gates AT, Graham DJ, Harper S, Hazuda DJ, Huang Q, McHale C, Monteagudo E, Pucci V, Rowley M, Rudd MT, Soriano A, Stahlhut MW, Vacca JP, Olsen DB, Liverton NJ, Carroll SS.

Antimicrob Agents Chemother. 2012 Aug;56(8):4161-7. doi: 10.1128/AAC.00324-12. Epub 2012 May 21. Erratum in: Antimicrob Agents Chemother. 2014 Aug;58(8):4995. Huang, Qian [added].

44.

Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.

Harper S, McCauley JA, Rudd MT, Ferrara M, DiFilippo M, Crescenzi B, Koch U, Petrocchi A, Holloway MK, Butcher JW, Romano JJ, Bush KJ, Gilbert KF, McIntyre CJ, Nguyen KT, Nizi E, Carroll SS, Ludmerer SW, Burlein C, DiMuzio JM, Graham DJ, McHale CM, Stahlhut MW, Olsen DB, Monteagudo E, Cianetti S, Giuliano C, Pucci V, Trainor N, Fandozzi CM, Rowley M, Coleman PJ, Vacca JP, Summa V, Liverton NJ.

ACS Med Chem Lett. 2012 Mar 2;3(4):332-6. doi: 10.1021/ml300017p. eCollection 2012 Apr 12.

45.

Challenges and opportunities in neuroscience research.

Coleman PJ, Barrow JC.

ChemMedChem. 2012 Mar 5;7(3):339-41. doi: 10.1002/cmdc.201200075. No abstract available.

PMID:
22383223
46.

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
47.

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
48.

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
49.

Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia.

Coleman PJ, Cox CD, Roecker AJ.

Curr Top Med Chem. 2011;11(6):696-725. Review.

PMID:
21261591
50.

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.

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