Search Results - "Reiss , Duane R."

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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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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Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure by Winrow, Christopher J., Tanis, Keith Q., Reiss, Duane R., Rigby, Alison M., Uslaner, Jason M., Uebele, Victor N., Doran, Scott M., Fox, Steven V., Garson, Susan L., Gotter, Anthony L., Levine, David M., Roecker, Anthony J., Coleman, Paul J., Koblan, Kenneth S., Renger, John J.

“…Orexin is a key neurotransmitter of central arousal and reward circuits in the CNS. Two receptors respond to orexin signaling, Orexin 1 Receptor (OX1R) and…”
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Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs) by Mercer, Swati P., Roecker, Anthony J., Garson, Susan, Reiss, Duane R., Meacham Harrell, C., Murphy, Kathy L., Bruno, Joseph G., Bednar, Rodney A., Lemaire, Wei, Cui, Donghui, Cabalu, Tamara D., Tang, Cuyue, Prueksaritanont, Thomayant, Hartman, George D., Young, Steven D., Winrow, Christopher J., Renger, John J., Coleman, Paul J.

“…The orexin (or hypocretin) system has been identified as a novel target for the treatment of insomnia due to the wealth of biological and genetic data…”
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Discovery of a Pharmacologically Active Antagonist of the Two-Pore-Domain Potassium Channel K2P9.1 (TASK-3) by Coburn, Craig A., Luo, Yunfu, Cui, Mingxiang, Wang, Jiabing, Soll, Richard, Dong, Jingchao, Hu, Bin, Lyon, Michael A., Santarelli, Vincent P., Kraus, Richard L., Gregan, Yun, Wang, Yi, Fox, Steven V., Binns, Jacquelyn, Doran, Scott M., Reiss, Duane R., Tannenbaum, Pamela L., Gotter, Anthony L., Meinke, Peter T., Renger, John J.

“…TWIK‐related acid‐sensitive K+ (K2P9.1, TASK‐3) ion channels have the capacity to regulate the activity of neuronal pathways by influencing the resting…”
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Discovery of a Potent, CNS‐Penetrant Orexin Receptor Antagonist Based on an N,N‐Disubstituted‐1,4‐diazepane Scaffold that Promotes Sleep in Rats by Whitman, David B., Cox, Christopher D., Breslin, Michael J., Brashear, Karen M., Schreier, John D., Bogusky, Michael J., Bednar, Rodney A., Lemaire, Wei, Bruno, Joseph G., Hartman, George D., Reiss , Duane R., Harrell, C. Meacham, Kraus, Richard L., Li, Yuxing, Garson, Susan L., Doran, Scott M., Prueksaritanont, Thomayant, Li, Chunze, Winrow, Christopher J., Koblan, Kenneth S., Renger, John J., Coleman, Paul J.

“…Silent Night: Antagonism of the orexin (or hypocretin) system has recently been identified as a novel mechanism for the treatment of insomnia. Herein, we…”
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Dual orexin receptor antagonists show distinct effects on locomotor performance, ethanol interaction and sleep architecture relative to gamma-aminobutyric acid-A receptor modulators by Ramirez, Andres D, Gotter, Anthony L, Fox, Steven V, Tannenbaum, Pamela L, Yao, Lihang, Tye, Spencer J, McDonald, Terrence, Brunner, Joseph, Garson, Susan L, Reiss, Duane R, Kuduk, Scott D, Coleman, Paul J, Uslaner, Jason M, Hodgson, Robert, Browne, Susan E, Renger, John J, Winrow, Christopher J

“…Dual orexin receptor antagonists (DORAs) are a potential treatment for insomnia that function by blocking both the orexin 1 and orexin 2 receptors. The…”
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Discovery of 3-Substituted Aminocyclopentanes as Potent and Orally Bioavailable NR2B Subtype-Selective NMDA Antagonists by Layton, Mark E., Kelly, Michael J., Rodzinak, Kevin J., Sanderson, Philip E., Young, Steven D., Bednar, Rodney A., DiLella, Anthony G., Mcdonald, Terrence P., Wang, Hao, Mosser, Scott D., Fay, John F., Cunningham, Michael E., Reiss, Duane R., Fandozzi, Christine, Trainor, Nicole, Liang, Annie, Lis, Edward V., Seabrook, Guy R., Urban, Mark O., Yergey, James, Koblan, Kenneth S.

“…A series of 3-substituted aminocyclopentanes has been identified as highly potent and selective NR2B receptor antagonists. Incorporation of a 1,2,4-oxadiazole…”
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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 by Coleman, Paul J., Schreier, John D., Cox, Christopher D., Breslin, Michael J., Whitman, David B., Bogusky, Michael J., McGaughey, Georgia B., Bednar, Rodney A., Lemaire, Wei, Doran, Scott M., Fox, Steven V., Garson, Susan L., Gotter, Anthony L., Harrell, C. Meacham, Reiss, Duane R., Cabalu, Tamara D., Cui, Donghui, Prueksaritanont, Thomayant, Stevens, Joanne, Tannenbaum, Pamela L., Ball, Richard G., Stellabott, Joyce, Young, Steven D., Hartman, George D., Winrow, Christopher J., Renger, John J.

“…Insomnia is a common disorder that can be comorbid with other physical and psychological illnesses. Traditional management of insomnia relies on general…”
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Antagonism of T-type calcium channels inhibits high-fat diet-induced weight gain in mice by Uebele, Victor N, Gotter, Anthony L, Nuss, Cindy E, Kraus, Richard L, Doran, Scott M, Garson, Susan L, Reiss, Duane R, Li, Yuxing, Barrow, James C, Reger, Thomas S, Yang, Zhi-Qiang, Ballard, Jeanine E, Tang, Cuyue, Metzger, Joseph M, Wang, Sheng-Ping, Koblan, Kenneth S, Renger, John J

“…The epidemics of obesity and metabolic disorders have well-recognized health and economic burdens. Pharmacologic treatments for these diseases remain…”
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TASK-3 as a potential antidepressant target by Gotter, Anthony L, Santarelli, Vincent P, Doran, Scott M, Tannenbaum, Pamela L, Kraus, Richard L, Rosahl, Thomas W, Meziane, Hamid, Montial, Marina, Reiss, Duane R, Wessner, Keith, McCampbell, Alexander, Stevens, Joanne, Brunner, Joseph I, Fox, Steven V, Uebele, Victor N, Bayliss, Douglas A, Winrow, Christopher J, Renger, John J

“…Abstract Modulation of TASK-3 ( Kcnk9 ) potassium channels affect neurotransmitter release in thalamocortical centers and other sleep-related nuclei having the…”
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Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat by Coleman, Paul J., Schreier, John D., Roecker, Anthony J., Mercer, Swati P., McGaughey, Georgia B., Cox, Christopher D., Hartman, George D., Harrell, C. Meacham, Reiss, Duane R., Doran, Scott M., Garson, Susan L., Anderson, Wayne B., Tang, Cuyue, Prueksaritanont, Thomayant, Winrow, Christopher J., Renger, John J.

“…In this Letter, we describe the synthesis of constrained diazepanes including 3,9-diazabicyclo[4.2.1]nonane 8a that has improved oral bioavailability and…”
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Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists by Melamed, Jeffrey Y., Zartman, Amy E., Kett, Nathan R., Gotter, Anthony L., Uebele, Victor N., Reiss, Duane R., Condra, Cindra L., Fandozzi, Christine, Lubbers, Laura S., Rowe, Blake A., McGaughey, Georgia B., Henault, Martin, Stocco, Rino, Renger, John J., Hartman, George D., Bilodeau, Mark T., Trotter, B. Wesley

“…Medicinal chemistry efforts have identified a quinolinone class of potent NPSR antagonists that readily cross the blood–brain barrier. Optimization efforts…”
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Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists by Coleman, Paul J., Schreier, John D., McGaughey, Georgia B., Bogusky, Michael J., Cox, Christopher D., Hartman, George D., Ball, Richard G., Harrell, C. Meacham, Reiss, Duane R., Prueksaritanont, Thomayant, Winrow, Christopher J., Renger, John J.

“…In this Letter we describe the design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as orexin receptor antagonists such as 8c…”
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Bradykinin B1 receptor antagonists : An α-hydroxy amide with an improved metabolism profile by KUDUK, Scott D, CHANG, Ronald K, BOCK, Mark G, DIPARDO, Robert M, DI MARCO, Christina N, MURPHY, Kathy L, RANSOM, Richard W, REISS, Duane R, TANG, Cuyue, PRUEKSARITANONT, Thomayant, PETTIBONE, Douglas J

“…A series of carbo- and heterocyclic alpha-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl alpha-hydroxy…”
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Development of Orally Bioavailable and CNS Penetrant Biphenylaminocyclopropane Carboxamide Bradykinin B1 Receptor Antagonists by Kuduk, Scott D., Di Marco, Christina N., Chang, Ronald K., Wood, Michael R., Schirripa, Kathy M., Kim, June J., Wai, Jenny M. C., DiPardo, Robert M., Murphy, Kathy L., Ransom, Richard W., Harrell, C. Meacham, Reiss, Duane R., Holahan, Marie A., Cook, Jacquelynn, Hess, J. Fred, Sain, Nova, Urban, Mark O., Tang, Cuyue, Prueksaritanont, Thomayant, Pettibone, Douglas J., Bock, Mark G.

“…A series of biphenylaminocyclopropane carboxamide based bradykinin B1 receptor antagonists has been developed that possesses good pharmacokinetic properties…”
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Indazole derivatives as novel bradykinin B1 receptor antagonists by BODMER-NARKEVITCH, Vera, ANTHONY, Neville J, BOCK, Mark G, KUDUK, Scott D, COFRE, Victoria, JOLLY, Samson M, MURPHY, Kathy L, RANSOM, Richard W, REISS, Duane R, CUYUE TANG, PRUEKSARITANONT, Thomayant, PETTIBONE, Douglas J

“…A new class of indazole-derived bradykinin B(1) antagonists and their structure-activity relationships (SAR) is reported. A number of compounds were found to…”
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Quantitative Proteomics in Laser Capture Microdissected Sleep Nuclei From Rat Brain by Miller, Ronald A., Winrow, Christopher J., Spellman, Daniel S., Song, Qinghua, Reiss, Duane R., Conway, James P., Taylor, Rhonda R., Coleman, Paul J., Hendrickson, Ronald C., Renger, John J.

“…Abstract The combination of stable isotope labeling of amino acids in mammals (SILAM) and laser capture microdissection (LCM) for selective proteomic analysis…”
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2-Aminobenzophenones as a Novel Class of Bradykinin B1 Receptor Antagonists by Su, Dai-Shi, Lim, John L, Tinney, Elizabeth, Wan, Bang-Lin, Murphy, Kathy L, Reiss, Duane R, Harrell, C. Meacham, O’Malley, Stacy S, Ransom, Rick W, Chang, Raymond S. L, Pettibone, Douglas J, Yu, Jian, Tang, Cuyue, Prueksaritanont, Thomayant, Freidinger, Roger M, Bock, Mark G, Anthony, Neville J

“…Selective bradykinin (BK) B1 receptor antagonists could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure…”
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Bradykinin B1 antagonists : Biphenyl SAR studies in the cyclopropanecarboxamide series by KUDUK, Scott D, DIPARDO, Robert M, BOCK, Mark G, CHANG, Ronald K, DI MARCO, Christina N, MURPHY, Kathy L, RANSOM, Richard W, REISS, Duane R, TANG, Cuyue, PRUEKSARITANONT, Thomayant, PETTIBONE, Douglas J

“…SAR study of the biphenyl region of cyclopropanecarboxamide derived bradykinin B(1) antagonists was examined. Incorporation of a pyridine in place of the…”
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