Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Susan L, Garson"'
Autor:
Pamela L. Tannenbaum, Joanne eStevens, Jacquelyn eBinns, Alan eSavitz, Susan L Garson, Steven V Fox, Paul eColeman, Scott D Kuduk, Anthony L Gotter, Michael eMarino, Spencer J Tye, Jason eUslaner, Christopher J Winrow, John J Renger
Publikováno v:
Frontiers in Behavioral Neuroscience, Vol 8 (2014)
The ability to awaken from sleep in response to important stimuli is a critical feature of normal sleep, as is maintaining sleep continuity in the presence of irrelevant background noise. Dual orexin receptor antagonists (DORAs) effectively promote s
Externí odkaz:
https://doaj.org/article/bc2e2cdd06ec407c9158c769a6c72cea
Autor:
Andres D. Ramirez, Anthony L. Gotter, Steven V. Fox, Pamela L. Tannenbaum, Lihang eYao, Spencer J. Tye, Terrence eMcDonald, Joseph eBrunner, Susan L. Garson, Duane R. Reiss, Scott D. Kuduk, Paul J. Coleman, Jason M. Uslaner, Robert eHodgson, Susan E. Browne, John J. Renger, Christopher J. Winrow
Publikováno v:
Frontiers in Neuroscience, Vol 7 (2013)
Dual orexin receptor antagonists (DORAs) are a potential treatment for insomnia that function by blocking both the orexin 1 and orexin 2 receptors. The objective of the current study was to further confirm the impact of therapeutic mechanisms targeti
Externí odkaz:
https://doaj.org/article/7a637e4e89e342579deeac811d80cf1d
Autor:
Christina N. DiMarco, Anthony L. Gotter, Alan T. Savitz, Joanne Stevens, Joseph G. Bruno, Tamara D. Cabalu, John J. Renger, Jason W. Skudlarek, Pamela L. Tannenbaum, Paul J. Coleman, Scott D. Kuduk, Joseph Brunner, Susan L. Garson, Christopher J. Winrow, Julie A. O'Brien, Charles M. Harrell, Mark H. Pausch
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2488-2492
Antagonism of orexin receptors has shown clinical efficacy as a novel paradigm for the treatment of insomnia and related disorders. Herein, molecules related to the dual orexin receptor antagonist filorexant were transformed into compounds that were
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7acadb1d22021c26105aca8a6acbc634
https://doi.org/10.1016/j.bmcl.2015.04.066
https://doi.org/10.1016/j.bmcl.2015.04.066
Autor:
Christopher J. Winrow, Joanne Stevens, Anthony J. Roecker, Charles M. Harrell, Alan T. Savitz, W. Peter Wuelfing, Kerim Babaoglu, Jason W. Skudlarek, Paul J. Coleman, Steven V. Fox, Christina Ng Dimarco, Pamela L. Tannenbaum, Scott D. Kuduk, Susan L. Garson, Joseph G. Bruno, Joseph Brunner, John J. Renger, Tamara D. Cabalu, Anthony L. Gotter, Mark A. Pausch, Julie A. O'Brien
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(6)
In an ongoing effort to explore the use of orexin receptor antagonists for the treatment of insomnia, dual orexin receptor antagonists (DORAs) were structurally modified, resulting in compounds selective for the OX2R subtype and culminating in the di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd5ac8c7f570e93f6ae4f582b7af1128
https://pubmed.ncbi.nlm.nih.gov/28216403
https://pubmed.ncbi.nlm.nih.gov/28216403
Autor:
John J. Renger, Joyce Stellabott, Swati P. Mercer, Wei Lemaire, Thomas S. Reger, Christopher D. Cox, Pamela L. Tannenbaum, Christopher J. Winrow, Joanne Stevens, Donghui Cui, Joseph G. Bruno, Susan L. Garson, Rowena V. Cube, M. Christa Mattern, Dansu Li, C. Meacham Harrell, Paul J. Coleman, John D. Schreier, Tamara D. Cabalu, George D. Hartman, Anthony L. Gotter, Steven V. Fox, Jeffrey M. Bergman, Anthony J. Roecker, Thomayant Prueksaritanont, Steven D. Young
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:4884-4890
Orexin receptor antagonists have demonstrated clinical utility for the treatment of insomnia. The majority of clinical efforts to date have focused on the development of dual orexin receptor antagonists (DORAs), small molecules that antagonize both t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9311b64883bbbf0739f9c64c3873b7ce
https://doi.org/10.1016/j.bmcl.2014.08.041
https://doi.org/10.1016/j.bmcl.2014.08.041
Autor:
Anthony L. Gotter, Vladimir Svetnik, Arie Struyk, Pamela L. Tannenbaum, Mark S. Forman, Nicole Calder, Susan L. Garson, John J. Renger, Christopher J. Winrow, Joanne Stevens, Anthony J. Roecker, Laura B. Rosen, W. Joseph Herring, Ka Lai Yee, Inge De Lepeleire, Xiaodong Li, Paul J. Coleman, Steven V. Fox, Charles M. Harrell
Publikováno v:
Scientific Reports
Orexin neuropeptides regulate sleep/wake through orexin receptors (OX1R, OX2R); OX2R is the predominant mediator of arousal promotion. The potential for single OX2R antagonism to effectively promote sleep has yet to be demonstrated in humans. MK-1064
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8f3bc3db6a5889a09f8b0e6f1bbba05
Autor:
Michael J. Breslin, Paul J. Coleman, Duane R. Reiss, Christopher D. Cox, Anthony L. Gotter, Joanne Stevens, Scott M. Doran, John D. Schreier, Donghui Cui, Christopher J. Winrow, John J. Renger, Steven V. Fox, Charles M. Harrell, Pamela L. Tannenbaum, Susan L. Garson
Publikováno v:
Neuropharmacology. 62:978-987
Orexin (hypocretin) neuropeptides promote wakefulness by signaling through two G-protein coupled receptors, Orexin 1 Receptor (OX(1)R) and Orexin 2 Receptor (OX(2)R). MK-6096 is an orally bioavailable potent and selective reversible antagonist of OX(
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d998ecd11613572c9ac99be809e4e4ff
https://doi.org/10.1016/j.neuropharm.2011.10.003
https://doi.org/10.1016/j.neuropharm.2011.10.003
Autor:
Rowena V. Cube, Cindy E. Nuss, Thomayant Prueksaritanont, Scott M. Doran, Jim Small, Wei Zeng, Julie Ann Luk, Cynthia Chavez-Eng, William O. Cook, T Laethem, Victor N. Uebele, Susan L. Garson, Thomas S. Reger, Richard L. Kraus, Yuhsin Kuo, Christa Mattern, Wei Fang, Cuyue Tang, John J. Renger, Paul J. Coleman, Kelly Ann S. Schlegel, Adekemi B. Taylor, Yuxing Li, Zhi Qiang Yang, James C. Barrow, Shu Youheng, Jeanine E. Ballard, Matthew D. Troyer, George D. Hartman, Steven V. Fox
Publikováno v:
ACS Medicinal Chemistry Letters. 1:504-509
A novel phenyl acetamide series of short-acting T-type calcium channel antagonists has been identified and evaluated using in vitro and in vivo assays. Heterocycle substitutions of the 4-position of the phenyl acetamides afforded potent and selective
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58657ea13446ca13430d01628baeb7b3
https://doi.org/10.1021/ml100170e
https://doi.org/10.1021/ml100170e
Autor:
Scott M. Doran, Kenneth E. Rittle, Yuxing Li, Cindy E. Nuss, Faith A. Mullen, Jeanine E. Ballard, Razvan Cristescu, Thomas S. Reger, Zhi-Qiang Yang, John J. Renger, Kenneth S. Koblan, Owen B. McManus, Vincent P. Santarelli, Rodney A. Bednar, Victor N. Uebele, Cuyue Tang, Susan L. Garson, Kelly-Ann S. Schlegel, Richard L. Kraus, Æ James C. Barrow, Ge Dai, Wei Lemaire, Steven V. Fox
Publikováno v:
Cell Biochemistry and Biophysics. 55:81-93
Low-voltage-activated (T-type) calcium channels play a role in diverse physiological responses including neuronal burst firing, hormone secretion, and cell growth. To better understand the biological role and therapeutic potential of the target, a nu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d29a9d226ba340e06a45f9ea741ba7e8
https://doi.org/10.1007/s12013-009-9057-4
https://doi.org/10.1007/s12013-009-9057-4
Autor:
John J. Renger, Chunze Li, Michael J. Bogusky, Yuxing Li, Scott M. Doran, David B. Whitman, Wei Lemaire, John D. Schreier, Joseph G. Bruno, Karen M. Brashear, Duane R. Reiss, Thomayant Prueksaritanont, Rodney A. Bednar, C. Meacham Harrell, Susan L. Garson, Paul J. Coleman, Richard L. Kraus, Christopher D. Cox, George D. Hartman, Kenneth S. Koblan, Michael J. Breslin, Christopher J. Winrow
Publikováno v:
ChemMedChem. 4:1069-1074
Silent Night: Antagonism of the orexin (or hypocretin) system has recently been identified as a novel mechanism for the treatment of insomnia. Herein, we describe discovery of a dual (OX(1)R/OX(2)R) orexin receptor antagonist featuring a 1,4-diazepan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e66d6f4c7866f587c095e4844466f8a6
https://doi.org/10.1002/cmdc.200900069
https://doi.org/10.1002/cmdc.200900069