Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Rosemarie Roeloffs"'
Autor:
Robert M, Owen, David, Blakemore, Lishuang, Cao, Neil, Flanagan, Rebecca, Fish, Karl R, Gibson, Rachel, Gurrell, Chan Woo, Huh, Juha, Kammonen, Elisabeth, Mortimer-Cassen, Sarah A, Nickolls, Kiyoyuki, Omoto, Dafydd, Owen, Andy, Pike, David C, Pryde, David S, Reynolds, Rosemarie, Roeloffs, Colin, Rose, Clara, Stead, Mifune, Takeuchi, Joseph S, Warmus, Christine, Watson
Publikováno v:
Journal of medicinal chemistry. 62(12)
The design, optimization, and evaluation of a series of novel imidazopyridazine-based subtype-selective positive allosteric modulators (PAMs) for the GABA
Autor:
Colin R. Rose, Elisabeth Mortimer-Cassen, Juha Kammonen, Rebecca L. Fish, David C. Pryde, Lishuang Cao, Sarah A. Nickolls, Neil J. Flanagan, Karl Richard Gibson, Joseph S. Warmus, Christine Anne Louise Watson, Chan Woo Huh, David J. Reynolds, Rachel Gurrell, Kiyoyuki Omoto, Andrew Pike, Clara Stead, David C. Blakemore, Rosemarie Roeloffs, Dafydd R. Owen, Mifune Takeuchi, Robert M. Owen
Publikováno v:
Journal of Medicinal Chemistry.
The design, optimization, and evaluation of a series of novel imidazopyridazine-based subtype-selective positive allosteric modulators (PAMs) for the GABAA ligand-gated ion channel are described. From a set of initial hits multiple subseries were des
Autor:
Rosemarie Roeloffs, Anthony W Bannon, Adam R. Brown, Alexandre J.C. Loucif, Aristos J. Alexandrou, Anthony J. Kirkup, Mathew D Fuller, Gillian Stockbridge, Edward B. Stevens, David Printzenhoff, Praveen Anand, Steve England, Claire Elizabeth Payne, Uma Anand, Peter J. Bungay, Aaron C. Gerlach, Mark L. Chapman, Kemp Mark Ian, John H. Mahoney, Rebecca L. Prime, Jonathon W Theile, Brett M Antonio, Richard P. Butt, Sharan K. Bagal
Publikováno v:
British Journal of Pharmacology. 172:2654-2670
Background and Purpose NaV1.8 ion channels have been highlighted as important molecular targets for the design of low MW blockers for the treatment of chronic pain. Here, we describe the effects of PF-01247324, a new generation, selective, orally bio
Autor:
Rosemarie Roeloffs, Brante P. Sampey, Bote G. Bruinsma, Shankar Ramaswamy, Lawrence T. Friedhoff, Harald Murck, Ebenezer Asare
Publikováno v:
Alzheimer's & Dementia. 13
Autor:
Rosemarie Roeloffs, Stephen Werness, Brian E. Marron, Chengmin Zhong, Brett Antonio, Ahmed H. Hakeem, Irene Drizin, Char-Chang Shieh, Mark L. Chapman, Joseph P. Mikusa, Marc J. C. Scanio, James B. Thomas, Shailen K. Joshi, Dong Liu, Mark A. Matulenko, Douglas S. Krafte, Robert N. Atkinson, Lei Shi, Kennan C. Marsh, Gricelda H. Simler, Matthew S Johnson, Michael J. Krambis, Kort Michael E, Michael F. Jarvis, Xu-Feng Zhang, Robert J. Gregg, Connie R. Faltynek, Matthew A. Secrest, Prisca Honore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6812-6815
A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Na(v)1.8 sodium channel is reported. Replacement of the furan nucleus and homologation of the anilide linker in subtype-selective blocker A-803467 (1
Autor:
Alan D. Wickenden, Paul Christopher Fritch, William Harrison, C Wesley Eargle, James F Burns, George Salvatore Amato, Grant Andrew Mcnaughton-Smith, Leslie Jones, Rosemarie Roeloffs
Publikováno v:
Journal of Medicinal Chemistry. 53:887-896
Current drugs for the treatment of seizure disorders, although effective in many patients, still suffer from a number of failures and are not effective in some forms of resistant epilepsies. Historically, many of these drugs have multiple mechanisms
Autor:
Xin Su, Brett Antonio, Rosemarie Roeloffs, James B. Thomas, Mark L. Chapman, Douglas S. Krafte, Neil A. Castle
Publikováno v:
Anesthesia & Analgesia. 109:632-640
BACKGROUND A non-opioid receptor-mediated inhibition of sodium channels in dorsal root ganglia (DRGs) by kappa-opioid receptor agonists (kappa-ORAs) has been reported to contribute to the antinociceptive actions in animals and humans. In this study,
Autor:
James O. McNamara, Greg C. Rigdon, Grant Andrew Mcnaughton-Smith, Stephen Werness, Rosemarie Roeloffs, James Stables, Christopher Crean, Neil Ghodadra, Alan D. Wickenden
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 326:818-828
Openers or activators of neuronal KCNQ2/Q3 potassium channels decrease neuronal excitability and may provide benefit in the treatment of disorders of neuronal excitability such as epilepsy. In the present study, we evaluate the effects of ICA-27243 [
Autor:
Matthew S Johnson, Dong Liu, Robert J. Gregg, Irene Drizin, Michael F. Gross, Gricelda Hernandez, Kennan C. Marsh, James B. Thomas, Mark L. Chapman, Chang Z. Zhu, Brian E. Marron, Connie R. Faltynek, Shailen K. Joshi, Prisca Honore, Stephen Werness, Michael E. Kort, Douglas S. Krafte, Robert N. Atkinson, Rosemarie Roeloffs, William A. Carroll, Marc J. C. Scanio, Xu-Feng Zhang, Donna M. Gauvin, Michael J. Krambis, Michael F. Jarvis, Char-Chang Shieh, Lei Shi, Joseph P. Mikusa
Publikováno v:
Bioorganic & Medicinal Chemistry. 16:6379-6386
The synthesis and pharmacological characterization of a novel furan-based class of voltage-gated sodium channel blockers is reported. Compounds were evaluated for their ability to block the tetrodotoxin-resistant sodium channel Na(v)1.8 (PN3) as well
Autor:
William A Carroll, Chengmin Zhong, Stephen Werness, Jinrong Liu, Matthew S Johnson, Lei Shi, Michael F Jarvis, James B. Thomas, Xu-Feng Zhang, Mark L. Chapman, Michael F. Gross, Shailen Joshi, Michael E. Kort, Marc J. C. Scanio, Dong Liu, Robert J Gregg, Rosemarie Roeloffs, Prisca Honore, Gricelda Hernandez, Gregory J Pacofsky, Douglas S. Krafte, Robert N. Atkinson, Brian E. Marron, Irene I. Drizin, Kennan C Marsh, Joseph P Mikusa, Michael J. Krambis, Bernard P Murray, Char-Chang Shieh, Connie R. Faltynek
Publikováno v:
Journal of Medicinal Chemistry. 51:407-416
Nav1.8 (also known as PN3) is a tetrodotoxin-resistant (TTx-r) voltage-gated sodium channel (VGSC) that is highly expressed on small diameter sensory neurons and has been implicated in the pathophysiology of inflammatory and neuropathic pain. Recent