Search Results - "Winrow, Christopher J."

Orexin Receptors: Pharmacology and Therapeutic Opportunities by SCAMMELL, Thomas E, WINROW, Christopher J

“…Orexin-A and -B (also known as hypocretin-1 and -2) are neuropeptides produced in the lateral hypothalamus that promote many aspects of arousal through the OX1…”
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International Union of Basic and Clinical Pharmacology. LXXXVI. Orexin receptor function, nomenclature and pharmacology by Gotter, Anthony L, Webber, Andrea L, Coleman, Paul J, Renger, John J, Winrow, Christopher J

“…Orexin signaling is essential for normal regulation of arousal and behavioral state control and represents an attractive target for therapeutics combating…”
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The Discovery of Suvorexant, the First Orexin Receptor Drug for Insomnia by Coleman, Paul J, Gotter, Anthony L, Herring, W. Joseph, Winrow, Christopher J, Renger, John J

“…Historically, pharmacological therapies have used mechanisms such as γ-aminobutyric acid A (GABA A ) receptor potentiation to drive sleep through broad…”
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Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors by Yin, Jie, Babaoglu, Kerim, Brautigam, Chad A, Clark, Lindsay, Shao, Zhenhua, Scheuermann, Thomas H, Harrell, Charles M, Gotter, Anthony L, Roecker, Anthony J, Winrow, Christopher J, Renger, John J, Coleman, Paul J, Rosenbaum, Daniel M

“…Human orexin receptors (hOX 1 R and hOX 2 R) are GPCRs involved in sleep regulation. Structures of hOX 1 R bound to a selective antagonist or to a dual…”
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Phelan-McDermid syndrome: a classification system after 30 years of experience by Phelan, Katy, Boccuto, Luigi, Powell, Craig M, Boeckers, Tobias M, van Ravenswaaij-Arts, Conny, Rogers, R Curtis, Sala, Carlo, Verpelli, Chiara, Thurm, Audrey, Bennett, Jr, William E, Winrow, Christopher J, Garrison, Sheldon R, Toro, Roberto, Bourgeron, Thomas

“…Phelan-McDermid syndrome (PMS) was initially called the 22q13 deletion syndrome based on its etiology as a deletion of the distal long arm of chromosome 22…”
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Evidence for orexinergic mechanisms in migraine by Hoffmann, Jan, Supronsinchai, Weera, Akerman, Simon, Andreou, Anna P, Winrow, Christopher J, Renger, John, Hargreaves, Richard, Goadsby, Peter J

“…Abstract Objective To examine the effect of the orexinergic blockade with a dual orexin receptor antagonist (DORA) on experimental models of peripheral and…”
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Distribution of histone deacetylases 1-11 in the rat brain by Broide, Ron S, Redwine, Jeff M, Aftahi, Najla, Young, Warren, Bloom, Floyd E, Winrow, Christopher J

“…Although protein phosphorylation has been characterized more extensively, modulation of the acetylation state of signaling molecules is now being recognized as…”
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Discovery of the Dual Orexin Receptor Antagonist [(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia by Cox, Christopher D, Breslin, Michael J, Whitman, David B, Schreier, John D, McGaughey, Georgia B, Bogusky, Michael J, Roecker, Anthony J, Mercer, Swati P, Bednar, Rodney A, Lemaire, Wei, Bruno, Joseph G, Reiss, Duane R, Harrell, C. Meacham, Murphy, Kathy L, Garson, Susan L, Doran, Scott M, Prueksaritanont, Thomayant, Anderson, Wayne B, Tang, Cuyue, Roller, Shane, Cabalu, Tamara D, Cui, Donghui, Hartman, George D, Young, Steven D, Koblan, Ken S, Winrow, Christopher J, Renger, John J, Coleman, Paul J

“…Despite increased understanding of the biological basis for sleep control in the brain, few novel mechanisms for the treatment of insomnia have been identified…”
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The CNS-penetrant soluble guanylate cyclase stimulator CYR119 attenuates markers of inflammation in the central nervous system by Correia, Susana S, Liu, Guang, Jacobson, Sarah, Bernier, Sylvie G, Tobin, Jenny V, Schwartzkopf, Chad D, Atwater, Emily, Lonie, Elisabeth, Rivers, Sam, Carvalho, Andrew, Germano, Peter, Tang, Kim, Iyengar, Rajesh R, Currie, Mark G, Hadcock, John R, Winrow, Christopher J, Jones, Juli E

“…Inflammation in the central nervous system (CNS) is observed in many neurological disorders. Nitric oxide-soluble guanylate cyclase-cyclic guanosine…”
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Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man by Gotter, Anthony L., Forman, Mark S., Harrell, Charles M., Stevens, Joanne, Svetnik, Vladimir, Yee, Ka Lai, Li, Xiaodong, Roecker, Anthony J., Fox, Steven V., Tannenbaum, Pamela L., Garson, Susan L., Lepeleire, Inge De, Calder, Nicole, Rosen, Laura, Struyk, Arie, Coleman, Paul J., Herring, W. Joseph, Renger, John J., Winrow, Christopher J.

“…Orexin neuropeptides regulate sleep/wake through orexin receptors (OX 1 R, OX 2 R); OX 2 R is the predominant mediator of arousal promotion. The potential for…”
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Orexin receptors as therapeutic drug targets by Gotter, Anthony L, Roecker, Anthony J, Hargreaves, Richard, Coleman, Paul J, Winrow, Christopher J, Renger, John J

“…Orexin (hypocretin) receptor antagonists stand as a model for the development of targeted CNS small-molecule therapeutics. The identification of mutations in…”
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Inhibition of Orexin Signaling Promotes Sleep Yet Preserves Salient Arousability in Monkeys by Tannenbaum, Pamela L, Tye, Spencer J, Stevens, Joanne, Gotter, Anthony L, Fox, Steven V, Savitz, Alan T, Coleman, Paul J, Uslaner, Jason M, Kuduk, Scott D, Hargreaves, Richard, Winrow, Christopher J, Renger, John J

“…In addition to enhancing sleep onset and maintenance, a desirable insomnia therapeutic agent would preserve healthy sleep's ability to wake and respond to…”
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Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia by Winrow, Christopher J., Gotter, Anthony L., Cox, Christopher D., Tannenbaum, Pamela L., Garson, Susan L., Doran, Scott M., Breslin, Michael J., Schreier, John D., Fox, Steven V., Harrell, Charles M., Stevens, Joanne, Reiss, Duane R., Cui, Donghui, Coleman, Paul J., Renger, John J.

“…Orexin (hypocretin) neuropeptides promote wakefulness by signaling through two G-protein coupled receptors, Orexin 1 Receptor (OX 1R) and Orexin 2 Receptor (OX…”
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The CNS-Penetrant Soluble Guanylate Cyclase Stimulator CY6463 Reveals its Therapeutic Potential in Neurodegenerative Diseases by Correia, Susana S., Iyengar, Rajesh R., Germano, Peter, Tang, Kim, Bernier, Sylvie G., Schwartzkopf, Chad D., Tobin, Jenny, Lee, Thomas W.-H., Liu, Guang, Jacobson, Sarah, Carvalho, Andrew, Rennie, Glen R., Jung, Joon, Renhowe, Paul A., Lonie, Elisabeth, Winrow, Christopher J., Hadcock, John R., Jones, Juli E., Currie, Mark G.

“…Effective treatments for neurodegenerative diseases remain elusive and are critically needed since the burden of these diseases increases across an aging…”
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Promotion of Sleep by Suvorexant-A Novel Dual Orexin Receptor Antagonist by Winrow, Christopher J., Gotter, Anthony L., Cox, Christopher D., Doran, Scott M., Tannenbaum, Pamela L., Breslin, Michael J., Garson, Susan L., Fox, Steven V., Harrell, Charles M., Stevens, Joanne, Reiss, Duane R., Cui, Donghui, Coleman, Paul J., Renger, John J.

“…Orexins/hypocretins are key neuropeptides responsible for regulating central arousal and reward circuits. Two receptors respond to orexin signaling, orexin 1…”
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The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold by Gotter, Anthony L, Winrow, Christopher J, Brunner, Joseph, Garson, Susan L, Fox, Steven V, Binns, Jacquelyn, Harrell, Charles M, Cui, Donghui, Yee, Ka Lai, Stiteler, Mark, Stevens, Joanne, Savitz, Alan, Tannenbaum, Pamela L, Tye, Spencer J, McDonald, Terrence, Yao, Leon, Kuduk, Scott D, Uslaner, Jason, Coleman, Paul J, Renger, John J

“…Drugs targeting insomnia ideally promote sleep throughout the night, maintain normal sleep architecture, and are devoid of residual effects associated with…”
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Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology by Stump, Craig A., Cooke, Andrew J., Bruno, Joseph, Cabalu, Tamara D., Gotter, Anthony L., Harell, C. Meacham, Kuduk, Scott D., McDonald, Terrence P., O’Brien, Julie, Renger, John J., Williams, Peter D., Winrow, Christopher J., Coleman, Paul J.

“…[Display omitted] While a correlation between blockade of the orexin 2 receptor (OX2R) with either a dual orexin receptor antagonist (DORA) or a selective…”
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The dual orexin receptor antagonist, DORA‐22, lowers histamine levels in the lateral hypothalamus and prefrontal cortex without lowering hippocampal acetylcholine by Yao, Lihang, Ramirez, Andres D., Roecker, Anthony J., Fox, Steven V., Uslaner, Jason M., Smith, Sean M., Hodgson, Robert, Coleman, Paul J., Renger, John J., Winrow, Christopher J., Gotter, Anthony L.

“…Chronic insomnia is defined as a persistent difficulty with sleep initiation maintenance or non‐restorative sleep. The therapeutic standard of care for this…”
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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 by Roecker, Anthony J., Mercer, Swati P., Schreier, John D., Cox, Christopher D., Fraley, Mark E., Steen, Justin T., Lemaire, Wei, Bruno, Joseph G., Harrell, C. Meacham, Garson, Susan L., Gotter, Anthony L., Fox, Steven V., Stevens, Joanne, Tannenbaum, Pamela L., Prueksaritanont, Thomayant, Cabalu, Tamara D., Cui, Donghui, Stellabott, Joyce, Hartman, George D., Young, Steven D., Winrow, Christopher J., Renger, John J., Coleman, Paul J.

“…The field of small‐molecule orexin antagonist research has evolved rapidly in the last 15 years from the discovery of the orexin peptides to clinical…”
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Discovery of MK-3697: A selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia by Roecker, Anthony J., Reger, Thomas S., Mattern, M. Christa, Mercer, Swati P., Bergman, Jeffrey M., Schreier, John D., Cube, Rowena V., Cox, Christopher D., Li, Dansu, Lemaire, Wei, Bruno, Joseph G., Harrell, C. Meacham, Garson, Susan L., Gotter, Anthony L., Fox, Steven V., Stevens, Joanne, Tannenbaum, Pamela L., Prueksaritanont, Thomayant, Cabalu, Tamara D., Cui, Donghui, Stellabott, Joyce, Hartman, George D., Young, Steven D., Winrow, Christopher J., Renger, John J., Coleman, Paul J.

“…MK-1064 was recently disclosed as a selective orexin 2 receptor antagonist (2-SORA) possessing a profile commensurate with clinical investigation for the…”
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