Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Brett M Antonio"'
Autor:
Talia A. Atkin, Chani M. Maher, Aaron C. Gerlach, Bryant C. Gay, Brett M. Antonio, Sonia C. Santos, Karen M. Padilla, JulieAnn Rader, Douglas S. Krafte, Matthew A. Fox, Gregory R. Stewart, Slavé Petrovski, Orrin Devinsky, Matthew Might, Steven Petrou, David B. Goldstein
Publikováno v:
Epilepsia. 59:802-813
Objective Many previous studies of drug repurposing have relied on literature review followed by evaluation of a limited number of candidate compounds. Here, we demonstrate the feasibility of a more comprehensive approach using high-throughput screen
Autor:
Christopher William West, Nigel Alan Swain, Peter J. Cox, Joseph S. Warmus, Kiyoyuki Omoto, David C. Pryde, George Salvatore Amato, Steven Michael Reister, Jamie Turner, Brett M Antonio, Aaron C. Gerlach, Brian E. Marron, Karen Padilla, Katrina Yoger, John H. Mahoney
Publikováno v:
ACS Medicinal Chemistry Letters. 8:666-671
A series of TRPA1 antagonists is described which has as its core structure an indazole moiety. The physical properties and in vitro DMPK profiles are discussed. Good in vivo exposure was obtained with several analogs, allowing efficacy to be assessed
Autor:
Sean, Ekins, Jacob, Gerlach, Kimberley M, Zorn, Brett M, Antonio, Zhixin, Lin, Aaron, Gerlach
Publikováno v:
Pharm Res
PURPOSE: Pitt Hopkins Syndrome (PTHS) is a rare genetic disorder caused by mutations of a specific gene, transcription factor 4 (TCF4), located on chromosome 18. PTHS results in individuals that have moderate to severe intellectual disability, with m
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:
Alexandre J C, Loucif, Pierre-Philippe, Saintot, Jia, Liu, Brett M, Antonio, Shannon G, Zellmer, Katrina, Yoger, Emma L, Veale, Anna, Wilbrey, Kiyoyuki, Omoto, Lishuang, Cao, Alex, Gutteridge, Neil A, Castle, Edward B, Stevens, Alistair, Mathie
Publikováno v:
British Journal of Pharmacology
Background and Purpose TREK two‐pore‐domain potassium (K2P) channels play a critical role in regulating the excitability of somatosensory nociceptive neurons and are important mediators of pain perception. An understanding of the roles of TREK ch
Autor:
Zhixin Lin, Mark L. Chapman, Christopher William West, Neil A. Castle, Stupple Paul Anthony, P. Kay Wagoner, Brett M Antonio, Marcel J. de Groot, Brian E. Marron, Richard P. Butt, Nigel Alan Swain, Ken McCormack, Sonia Santos, Shannon G. Zellmer, David Printzenhoff, Karen Padilla, Michael J. Krambis, Douglas S. Krafte
Publikováno v:
Proceedings of the National Academy of Sciences. 110
Voltage-gated sodium (Nav) channels play a fundamental role in the generation and propagation of electrical impulses in excitable cells. Here we describe two unique structurally related nanomolar potent small molecule Nav channel inhibitors that exhi