Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Jonathan W Theile"'
Publikováno v:
eLife, Vol 11 (2022)
Resurgent currents (INaR) produced by voltage-gated sodium channels are required for many neurons to maintain high-frequency firing and contribute to neuronal hyperexcitability and disease pathophysiology. Here, we show, for the first time, that INaR
Externí odkaz:
https://doaj.org/article/9523fdcf8a444e838dc5323b8a3e17e1
Autor:
Rhianna E. Lee, Catherine A. Lewis, Lihua He, Emily C. Bulik-Sullivan, Samuel C. Gallant, Teresa M. Mascenik, Hong Dang, Deborah M. Cholon, Martina Gentzsch, Lisa C. Morton, John T. Minges, Jonathan W. Theile, Neil A. Castle, Michael R. Knowles, Adam J. Kimple, Scott H. Randell
Publikováno v:
The Journal of Clinical Investigation, Vol 132, Iss 18 (2022)
The vast majority of people with cystic fibrosis (CF) are now eligible for CF transmembrane regulator (CFTR) modulator therapy. The remaining individuals with CF harbor premature termination codons (PTCs) or rare CFTR variants with limited treatment
Externí odkaz:
https://doaj.org/article/0342006f024949bb976f55db34ef1e17
Autor:
Jonathan W. Theile, Theodore R Cummins
Publikováno v:
Frontiers in Pharmacology, Vol 2 (2011)
Chronic and neuropathic pain constitute significant health problems affecting millions of individuals each year. Pain sensations typically originate in sensory neurons of the peripheral nervous system (PNS) which relay information to the central nerv
Externí odkaz:
https://doaj.org/article/af3183f563da43d2a7dc47ce6acc6a5b
Autor:
Jianmin Sun, Thomas Ryckmans, David Fengas, Colin R. Rose, M. Scott Johnson, Matthew Corbett, David James Rawson, Nigel Alan Swain, Joseph S. Warmus, Lyn H. Jones, Brian E. Marron, Aristos J. Alexandrou, David Printzenhoff, C. Elizabeth Payne, Bruce M. Bechle, Rubben Torella, Neil A. Castle, Jonathan W. Theile, Elaine Tseng, David C. Blakemore, Andrew Pike, R. Ian Storer, Neil J. Flanagan, Alan Daniel Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:4805-4811
The discovery and selection of a highly potent and selective NaV1.7 inhibitor PF-06456384, designed specifically for intravenous infusion, is disclosed. Extensive in vitro pharmacology and ADME profiling followed by in vivo preclinical PK and efficac
Publikováno v:
Molecular Pharmacology. 90:540-548
Voltage-gated sodium (Nav) channel inhibitors are used clinically as analgesics and local anesthetics. However, the absence of Nav channel isoform selectivity of current treatment options can result in adverse cardiac and central nervous system side
Autor:
R Ian, Storer, Andy, Pike, Nigel A, Swain, Aristos J, Alexandrou, Bruce M, Bechle, David C, Blakemore, Alan D, Brown, Neil A, Castle, Matthew S, Corbett, Neil J, Flanagan, David, Fengas, M Scott, Johnson, Lyn H, Jones, Brian E, Marron, C Elizabeth, Payne, David, Printzenhoff, David J, Rawson, Colin R, Rose, Thomas, Ryckmans, Jianmin, Sun, Jonathan W, Theile, Rubben, Torella, Elaine, Tseng, Joseph S, Warmus
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(21)
The discovery and selection of a highly potent and selective Na
Publikováno v:
Molecular Pharmacology. 80:724-734
Paroxysmal extreme pain disorder (PEPD) and inherited erythromelalgia (IEM) are inherited pain syndromes arising from different sets of gain-of-function mutations in the sensory neuronal sodium channel isoform Nav1.7. Mutations associated with PEPD,
Publikováno v:
The Journal of Physiology. 589:597-608
Abnormal pain sensitivity associated with inherited and acquired pain disorders occurs through increased excitability of peripheral sensory neurons in part due to changes in the properties of voltage-gated sodium channels (Navs). Resurgent sodium cur
Publikováno v:
Neuroscience. 172:94-103
Activation of the dopaminergic (DA) neurons of the ventral tegmental area (VTA) by ethanol has been implicated in its rewarding and reinforcing effects. We previously demonstrated that ethanol enhances GABA release onto VTA-DA neurons via activation