Michael F. Gross
Research Triangle Park
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Publication
Featured researches published by Michael F. Gross.
Journal of Medicinal Chemistry | 2008
Michael E. Kort; Irene Drizin; Robert J. Gregg; Marc Scanio; Lei Shi; Michael F. Gross; Robert Nelson Atkinson; Matthew S. Johnson; Gregory J. Pacofsky; James B. Thomas; William A. Carroll; Michael J. Krambis; Dong Liu; Char-Chang Shieh; Xu-Feng Zhang; Gricelda Hernandez; Joseph P. Mikusa; Chengmin Zhong; Shailen K. Joshi; Prisca Honore; Rosemarie Roeloffs; Kennan C. Marsh; Bernard P. Murray; Jinrong Liu; Stephen Werness; Connie R. Faltynek; Douglas S. Krafte; Michael F. Jarvis; Mark L. Chapman; Brian Edward Marron
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 studies using an Nav1.8 antisense oligonucleotide in an animal model of chronic pain indicated that selective blockade of Nav1.8 was analgesic and could provide effective analgesia with a reduction in the adverse events associated with nonselective VGSC blocking therapeutic agents. Herein, we describe the preparation and characterization of a series of 5-substituted 2-furfuramides, which are potent, voltage-dependent blockers (IC50 < 10 nM) of the human Nav1.8 channel. Selected derivatives, such as 7 and 27, also blocked TTx-r sodium currents in rat dorsal root ganglia (DRG) neurons with comparable potency and displayed >100-fold selectivity versus human sodium (Nav1.2, Nav1.5, Nav1.7) and human ether-a-go-go (hERG) channels. Following systemic administration, compounds 7 and 27 dose-dependently reduced neuropathic and inflammatory pain in experimental rodent models.
Bioorganic & Medicinal Chemistry Letters | 2009
Michael F. Gross; Neil A. Castle; Anruo Zou; Alan D. Wickenden; Weifeng Yu; Kerry L. Spear
Aryl sulfonamido tetralins based on lead compound 2a were synthesized and evaluated for Kv1.5 inhibitory activity. Several compounds having IC(50) values less then 0.1 microM were identified. Kv1.5 inhibitors have the potential to be atrium-selective agents for the treatment of atrial fibrillation.
Archive | 2002
Robert Nelson Atkinson; Michael F. Gross
Archive | 1999
John Lloyd; Heather Finlay; Wayne Vaccaro; Karnail S. Atwal; Michael F. Gross; Kerry L. Spear
Archive | 2000
Alan D. Wickenden; Gregory Cooksey Rigdon; Grant McNaughton-Smith; Michael F. Gross
Bioorganic & Medicinal Chemistry Letters | 2007
Michael F. Gross; Serge Beaudoin; Grant McNaughton-Smith; George S. Amato; Neil A. Castle; Christine Huang; Anruo Zou; Weifeng Yu
Archive | 2004
Robert Nelson Atkinson; Irene Drizin; Robert J. Gregg; Michael F. Gross; Michael E. Kort; Lei Shi
Archive | 2005
Michael F. Gross; John Lloyd
Archive | 2005
Michael F. Gross; John Lloyd
Archive | 2003
John Lloyd; Yoon T. Jeon; Heather Finlay; Lin Yan; Michael F. Gross; Serge Beaudoin