Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1. 8 sodium channel with efficacy in models of neuropathic and …

…, RN Atkinson, MS Johnson, GJ Pacofsky…

文献索引：Kort, Michael E.; Drizin, Irene; Gregg, Robert J.; Scanio, Marc J. C.; Shi, Lei; Gross, Michael F.; Atkinson, Robert N.; Johnson, Matthew S.; Pacofsky, Gregory J.; Thomas, James B.; Carroll, William A.; Krambis, Michael J.; Liu, Dong; Shieh, Char-Chang; Zhang, XuFeng; Hernandez, Gricelda; Mikusa, Joseph P.; Zhong, Chengmin; Joshi, Shailen; Honore, Prisca; Roeloffs, Rosemarie; Marsh, Kennan C.; Murray, Bernard P.; Liu, Jinrong; Werness, Stephen; Faltynek, Connie R.; Krafte, Douglas S.; Jarvis, Michael F.; Chapman, Mark L.; Marron, Brian E. Journal of Medicinal Chemistry, 2008 , vol. 51, # 3 p. 407 - 416

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被引用次数: 66

摘要

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 ...