Search Results - "Printzenhoff, David"

Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release by Alexandrou, Aristos J, Brown, Adam R, Chapman, Mark L, Estacion, Mark, Turner, Jamie, Mis, Malgorzata A, Wilbrey, Anna, Payne, Elizabeth C, Gutteridge, Alex, Cox, Peter J, Doyle, Rachel, Printzenhoff, David, Lin, Zhixin, Marron, Brian E, West, Christopher, Swain, Nigel A, Storer, R Ian, Stupple, Paul A, Castle, Neil A, Hounshell, James A, Rivara, Mirko, Randall, Andrew, Dib-Hajj, Sulayman D, Krafte, Douglas, Waxman, Stephen G, Patel, Manoj K, Butt, Richard P, Stevens, Edward B

“…Human genetic studies show that the voltage gated sodium channel 1.7 (Nav1.7) is a key molecular determinant of pain sensation. However, defining the Nav1.7…”
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Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels by McCormack, Ken, Santos, Sonia, Chapman, Mark L, Krafte, Douglas S, Marron, Brian E, West, Christopher W, Krambis, Michael J, Antonio, Brett M, Zellmer, Shannon G, Printzenhoff, David, Padilla, Karen M, Lin, Zhixin, Wagoner, P Kay, Swain, Nigel A, Stupple, Paul A, de Groot, Marcel, Butt, Richard P, Castle, Neil A

“…Voltage-gated sodium (Na ᵥ) channels play a fundamental role in the generation and propagation of electrical impulses in excitable cells. Here we describe two…”
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Biophysical and Pharmacological Characterization of Nav1.9 Voltage Dependent Sodium Channels Stably Expressed in HEK-293 Cells by Lin, Zhixin, Santos, Sonia, Padilla, Karen, Printzenhoff, David, Castle, Neil A

“…The voltage dependent sodium channel Nav1.9, is expressed preferentially in peripheral sensory neurons and has been linked to human genetic pain disorders,…”
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PF‐06526290 can both enhance and inhibit conduction through voltage‐gated sodium channels by Wang, Lingxin, Zellmer, Shannon G, Printzenhoff, David M, Castle, Neil A

“…Background and Purpose Pharmacological agents that either inhibit or enhance flux of ions through voltage‐gated sodium (Nav) channels may provide opportunities…”
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A novel selective and orally bioavailable Nav1.8 channel blocker, PF‐01247324, attenuates nociception and sensory neuron excitability by Payne, Claire Elizabeth, Brown, Adam R, Theile, Jonathon W, Loucif, Alexandre J C, Alexandrou, Aristos J, Fuller, Mathew D, Mahoney, John H, Antonio, Brett M, Gerlach, Aaron C, Printzenhoff, David M, Prime, Rebecca L, Stockbridge, Gillian, Kirkup, Anthony J, Bannon, Anthony W, England, Steve, Chapman, Mark L, Bagal, Sharan, Roeloffs, Rosemarie, Anand, Uma, Anand, Praveen, Bungay, Peter J, Kemp, Mark, Butt, Richard P, Stevens, Edward B

“…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…”
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Addition of a single methyl group to a small molecule sodium channel inhibitor introduces a new mode of gating modulation by Wang, Lingxin, Zellmer, Shannon G, Printzenhoff, David M, Castle, Neil A

“…Aryl sulfonamide Nav 1.3 or Nav 1.7 voltage-gated sodium (Nav ) channel inhibitors interact with the Domain 4 voltage sensor domain (D4 VSD). During studies to…”
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Retracted: Addition of a single methyl group to a small molecule sodium channel inhibitor introduces a new mode of gating modulation by Wang, Lingxin, Zellmer, Shannon G., Printzenhoff, David M., Castle, Neil A.

“…Background and Purpose Aryl sulfonamide Nav1.3 or Nav1.7 voltage‐gated sodium (Nav) channel inhibitors interact with the Domain 4 voltage sensor domain (D4…”
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Sodium channel inhibitor drug discovery using automated high throughput electrophysiology platforms by Castle, Neil, Printzenhoff, David, Zellmer, Shannon, Antonio, Brett, Wickenden, Alan, Silvia, Christopher

“…Voltage dependent sodium channels are widely recognized as valuable targets for the development of therapeutic interventions for neuroexcitatory disorders such…”
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Discovery of Clinical Candidate 4‑[2-(5-Amino‑1H‑pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro‑N‑1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7 by Swain, Nigel. A, Batchelor, Dave, Beaudoin, Serge, Bechle, Bruce M, Bradley, Paul A, Brown, Alan D, Brown, Bruce, Butcher, Ken J, Butt, Richard P, Chapman, Mark L, Denton, Stephen, Ellis, David, Galan, Sebastien R. G, Gaulier, Steven M, Greener, Ben S, de Groot, Marcel J, Glossop, Mel S, Gurrell, Ian K, Hannam, Jo, Johnson, Matthew S, Lin, Zhixin, Markworth, Christopher J, Marron, Brian E, Millan, David S, Nakagawa, Shoko, Pike, Andy, Printzenhoff, David, Rawson, David J, Ransley, Sarah J, Reister, Steven M, Sasaki, Kosuke, Storer, R. Ian, Stupple, Paul A, West, Christopher W

“…A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective NaV1.7 inhibitors is described. Optimization of early lead…”
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Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes by Storer, R. Ian, Pike, Andy, Swain, Nigel A., Alexandrou, Aristos J., Bechle, Bruce M., Blakemore, David C., Brown, Alan D., Castle, Neil A., Corbett, Matthew S., Flanagan, Neil J., Fengas, David, Johnson, M. Scott, Jones, Lyn H., Marron, Brian E., Payne, C. Elizabeth, Printzenhoff, David, Rawson, David J., Rose, Colin R., Ryckmans, Thomas, Sun, Jianmin, Theile, Jonathan W., Torella, Rubben, Tseng, Elaine, Warmus, Joseph S.

“…[Display omitted] The discovery and selection of a highly potent and selective NaV1.7 inhibitor PF-06456384, designed specifically for intravenous infusion, is…”
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Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na V 1.7 by Swain, Nigel A, Batchelor, Dave, Beaudoin, Serge, Bechle, Bruce M, Bradley, Paul A, Brown, Alan D, Brown, Bruce, Butcher, Ken J, Butt, Richard P, Chapman, Mark L, Denton, Stephen, Ellis, David, Galan, Sebastien R G, Gaulier, Steven M, Greener, Ben S, de Groot, Marcel J, Glossop, Mel S, Gurrell, Ian K, Hannam, Jo, Johnson, Matthew S, Lin, Zhixin, Markworth, Christopher J, Marron, Brian E, Millan, David S, Nakagawa, Shoko, Pike, Andy, Printzenhoff, David, Rawson, David J, Ransley, Sarah J, Reister, Steven M, Sasaki, Kosuke, Storer, R Ian, Stupple, Paul A, West, Christopher W

“…A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective Na 1.7 inhibitors is described. Optimization of early lead…”
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A novel selective and orally bioavailable N a v 1.8 channel blocker, PF ‐01247324, attenuates nociception and sensory neuron excitability by Payne, Claire Elizabeth, Brown, Adam R, Theile, Jonathon W, Loucif, Alexandre J C, Alexandrou, Aristos J, Fuller, Mathew D, Mahoney, John H, Antonio, Brett M, Gerlach, Aaron C, Printzenhoff, David M, Prime, Rebecca L, Stockbridge, Gillian, Kirkup, Anthony J, Bannon, Anthony W, England, Steve, Chapman, Mark L, Bagal, Sharan, Roeloffs, Rosemarie, Anand, Uma, Anand, Praveen, Bungay, Peter J, Kemp, Mark, Butt, Richard P, Stevens, Edward B

“…Background and Purpose N a V 1.8 ion channels have been highlighted as important molecular targets for the design of low MW blockers for the treatment of…”
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A novel selective and orally bioavailable Na sub(v)1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability by Payne, Claire Elizabeth, Brown, Adam R, Theile, Jonathon W, Loucif, Alexandre J C, Alexandrou, Aristos J, Fuller, Mathew D, Mahoney, John H, Antonio, Brett M, Gerlach, Aaron C, Printzenhoff, David M, Prime, Rebecca L, Stockbridge, Gillian, Kirkup, Anthony J, Bannon, Anthony W, England, Steve, Chapman, Mark L, Bagal, Sharan, Roeloffs, Rosemarie, Anand, Uma, Anand, Praveen, Bungay, Peter J, Kemp, Mark, Butt, Richard P, Stevens, Edward B

“…Background and Purpose Na sub(V)1.8 ion channels have been highlighted as important molecular targets for the design of low MW blockers for the treatment of…”
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Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels by McCormack, Ken, Santos, Sonia, Chapman, Mark L., Krafte, Douglas S., Marron, Brian E., West, Christopher W., Krambis, Michael J., Antonio, Brett M., Zellmer, Shannon G., Printzenhoff, David, Padilla, Karen M., Lin, Zhixin, Wagoner, P. Kay, Swain, Nigel A., Stupple, Paul A., de Groot, Marcel, Butt, Richard P., Castle, Neil A.

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Highly potent and selective Na V 1.7 inhibitors for use as intravenous agents and chemical probes by Storer, R Ian, Pike, Andy, Swain, Nigel A, Alexandrou, Aristos J, Bechle, Bruce M, Blakemore, David C, Brown, Alan D, Castle, Neil A, Corbett, Matthew S, Flanagan, Neil J, Fengas, David, Johnson, M Scott, Jones, Lyn H, Marron, Brian E, Payne, C Elizabeth, Printzenhoff, David, Rawson, David J, Rose, Colin R, Ryckmans, Thomas, Sun, Jianmin, Theile, Jonathan W, Torella, Rubben, Tseng, Elaine, Warmus, Joseph S

“…The discovery and selection of a highly potent and selective Na 1.7 inhibitor PF-06456384, designed specifically for intravenous infusion, is disclosed…”
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A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability by Payne, Claire Elizabeth, Brown, Adam R, Theile, Jonathon W, Loucif, Alexandre J C, Alexandrou, Aristos J, Fuller, Mathew D, Mahoney, John H, Antonio, Brett M, Gerlach, Aaron C, Printzenhoff, David M, Prime, Rebecca L, Stockbridge, Gillian, Kirkup, Anthony J, Bannon, Anthony W, England, Steve, Chapman, Mark L, Bagal, Sharan, Roeloffs, Rosemarie, Anand, Uma, Anand, Praveen, Bungay, Peter J, Kemp, Mark, Butt, Richard P, Stevens, Edward B

“…NaV 1.8 ion channels have been highlighted as important molecular targets for the design of low MW blockers for the treatment of chronic pain. Here, we…”
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Tenidap, a novel anti-inflammatory agent, is an opener of the inwardly rectifying K + channel hKir2.3 by Liu, Yi, Liu, Dong, Printzenhoff, David, Coghlan, Michael J., Harris, Richard, Krafte, Douglas S.

“…We studied the effect of a novel anti-inflammatory agent, tenidap, on a cloned inwardly rectifying K + channel, hKir2.3. Tenidap (a) potently potentiated 86Rb…”
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In vitro and in vivo characterization of a novel naphthylamide ATP‐sensitive K+ channel opener, A‐151892 by Gopalakrishnan, Murali, Buckner, Steven A, Shieh, Char‐Chang, Fey, Thomas, Fabiyi, Adebola, Whiteaker, Kristi L, Davis‐Taber, Rachel, Milicic, Ivan, Daza, Anthony V, Scott, Victoria E S, Castle, Neil A, Printzenhoff, David, London, Brecht, Turner, Sean C, Carroll, William A, Sullivan, James P, Coghlan, Michael J, Brune, Michael E

“…Openers of ATP‐sensitive K+ channels are of interest in several therapeutic indications including overactive bladder and other lower urinary tract disorders…”
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Retrospective Analysis of an Experimental High-Throughput Screening Data Set by Recursive Partitioning by van Rhee, A. Michiel, Stocker, Jon, Printzenhoff, David, Creech, Chris, Wagoner, P. Kay, Spear, Kerry L

“…With the emergence of combinatorial chemistry, whether based on parallel, mixture, solution, or solid phase chemistry, it is now possible to generate large…”
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