Zobrazeno 1 - 10
of 61
pro vyhledávání: '"Darrell A. Henze"'
Autor:
Rebecca M. Klein, Mark E. Layton, Hillary Regan, Christopher P. Regan, Yuxing Li, Tracey Filzen, Matt Cato, Michelle K. Clements, Jixin Wang, Raul Sanoja, Thomas J. Greshock, Anthony J. Roecker, Joseph E. Pero, Ron Kim, Christopher Burgey, Christopher T. John, Ying-Hong Wang, Neetesh Bhandari, Arie Struyk, Richard L. Kraus, Darrell A. Henze, Andrea K. Houghton
Publikováno v:
Channels, Vol 16, Iss 1, Pp 230-243 (2022)
As part of a drug discovery effort to identify potent inhibitors of NaV1.7 for the treatment of pain, we observed that inhibitors produced unexpected cardiovascular and respiratory effects in vivo. Specifically, inhibitors administered to rodents pro
Externí odkaz:
https://doaj.org/article/55057518620746559c951066d12dfcf1
Autor:
Jeanine E. Ballard, Parul S. Pall, Joshua Vardigan, Fuqiang Zhao, Marie A. Holahan, Xiaoping Zhou, Nina Jochnowitz, Richard L. Kraus, Rebecca M. Klein, Darrell A. Henze, Andrea K. Houghton, Christopher S. Burgey, Christopher Gibson, Arie Struyk
Publikováno v:
Frontiers in Pharmacology, Vol 12 (2021)
MK-2075 is a small-molecule selective inhibitor of the NaV1.7 channel investigated for the treatment of postoperative pain. A translational strategy was developed for MK-2075 to quantitatively interrelate drug exposure, target modulation, and the des
Externí odkaz:
https://doaj.org/article/b6acf3025c844a49ac376ac7097521ef
Autor:
Gregory L. Adams, Parul S. Pall, Steven M. Grauer, Xiaoping Zhou, Jeanine E. Ballard, Marissa Vavrek, Richard L. Kraus, Pierre Morissette, Nianyu Li, Stefania Colarusso, Elisabetta Bianchi, Anandan Palani, Rebecca Klein, Christopher T. John, Deping Wang, Matthew Tudor, Andrew F. Nolting, Mirlinda Biba, Timothy Nowak, Alexey A. Makarov, Mikhail Reibarkh, Alexei V. Buevich, Wendy Zhong, Erik L. Regalado, Xiao Wang, Qi Gao, Aurash Shahripour, Yuping Zhu, Daniele de Simone, Tommaso Frattarelli, Nicolo’ Maria Pasquini, Paola Magotti, Roberto Iaccarino, Yuxing Li, Kelli Solly, Keun-Joong Lee, Weixun Wang, Feifei Chen, Haoyu Zeng, Jixin Wang, Hilary Regan, Rupesh P. Amin, Christopher P. Regan, Christopher S. Burgey, Darrell A. Henze, Chengzao Sun, David M. Tellers
Publikováno v:
Journal of Medicinal Chemistry. 65:485-496
Autor:
Richard L. Kraus, Ronald M. Kim, Jeanine E. Ballard, Thomas J. Greshock, Andrea K. Houghton, Michelle K. Clements, Marie A. Holahan, Andrew Danziger, Christopher S. Burgey, Yuxing Li, Mark E. Layton, Jordi Serra, Parul S. Pall, Rebecca M. Klein, Joshua D. Vardigan, Dan Zhou, Fuqiang Zhao, Christopher Daley, Darrell A. Henze
Publikováno v:
Science Translational Medicine. 13
Humans with loss-of-function mutations in the Nav1.7 channel gene (SCN9A) show profound insensitivity to pain, whereas those with gain-of-function mutations can have inherited pain syndromes. Therefore, inhibition of the Nav1.7 channel with a small m
Autor:
Joshua D. Vardigan, Christopher R. Gibson, Darrell A. Henze, Andrea K. Houghton, Marie A. Holahan, Fuqiang Zhao, Parul S. Pall, Richard L. Kraus, Yuxing Li, Jeanine E. Ballard, Christopher S. Burgey
Publikováno v:
Pharmaceutical Research
Purpose This work describes a staged approach to the application of pharmacokinetic-pharmacodynamic (PK-PD) modeling in the voltage-gated sodium ion channel (NaV1.7) inhibitor drug discovery effort to address strategic questions regarding in vitro to
Autor:
Darrell A. Henze, Joshua D. Vardigan, Vanita Puri, Christopher E. Cannon, Jason M. Uslaner, Henry S. Lange
Publikováno v:
Neuropharmacology. 197:108754
Alzheimer's disease (AD) is a profoundly debilitating neurodegenerative disorder characterized most notably by progressive cognitive decline, but also agitation and behavioral disturbances that are extremely disruptive to patient and caregiver. Curre
Autor:
Andrea K. Houghton, Aneta Jovanovska, Tracey Filzen, Ying-Hong Wang, Jacqueline Panigel, Annie Liang, Michelle K. Clements, Rebecca M. Klein, Richard L. Kraus, John Majercak, Eleftheria N. Finger, Jixin Wang, Matthew J. Cato, Hannah D. G. F. Lehman, Christopher Daley, Yun Gregan, James Mulhearn, Yuxing Li, Michael A. Rossi, Darrell A. Henze, Mark O. Urban, Michael J. Kelly, Scott E. Wolkenberg, Mark E. Layton, Joseph E. Pero
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:2683-2688
Studies on human genetics have suggested that inhibitors of the Nav1.7 voltage-gated sodium channel hold considerable promise as therapies for the treatment of chronic pain syndromes. Herein, we report novel, peripherally-restricted benzoxazolinone a
Publikováno v:
Journal of Neuroscience Methods. 282:34-42
Background NGF signaling through TrkA triggers pathways involved in a wide range of biological effects. Clinical trials targeting either NGF or TrkA are ongoing to treat various diseases in the areas of oncology, neuroscience, and for pain, but there
Autor:
Richard L, Kraus, Fuqiang, Zhao, Parul S, Pall, Dan, Zhou, Joshua D, Vardigan, Andrew, Danziger, Yuxing, Li, Christopher, Daley, Jeanine E, Ballard, Michelle K, Clements, Rebecca M, Klein, Marie A, Holahan, Thomas J, Greshock, Ronald M, Kim, Mark E, Layton, Christopher S, Burgey, Jordi, Serra, Darrell A, Henze, Andrea K, Houghton
Publikováno v:
Science translational medicine. 13(594)
Humans with loss-of-function mutations in the Na
Autor:
John A. Morrow, Raul Sanoja, Jacob Marcus, Daniel Zwilling, Darrell A. Henze, Nina Jochnowitz, Christopher Mittlelhaeuser, Robert Mazzola, Michael Calhoun, Hamid Meziane, Harunor Rashid, Dominic Poulin, Sean M. Smith, Thomas W. Rosahl, Geoffrey B. Varty, Steven M. Grauer
Publikováno v:
Brain Research. 1737:146814
Analgesic properties of orthosteric agonists of the muscarinic M4 receptor subtype have been documented in literature reports, with evidence from pharmacological and in vivo receptor knock out (KO) studies. Constitutive M4 receptor KO mice demonstrat