Results 221 to 230 of about 9,275 (242)

Small molecule targeting NaV1.7 via inhibition of CRMP2-Ubc9 interaction reduces pain-related outcomes in a rodent osteoarthritic model.

Pain
Osteoarthritis (OA) is a highly prevalent and disabling joint disease, characterized by pathological progressive joint deformation and clinical symptoms of pain.
Sara Hestehave, Heather N. Allen, Kimberly Gomez, Paz Duran, Aida Calderon-Rivera, Santiago Loya-López, Erick J. Rodríguez-Palma, R. Khanna   +7 more
semanticscholar   +1 more source

Reduction of SIRT1-Mediated Epigenetic Upregulation of Nav1.7 Contributes to Oxaliplatin-Induced Neuropathic Pain.

Pain Physician, 2023
BACKGROUND Clinically, neuropathic pain is a severe side effect of oxaliplatin chemotherapy, which usually leads to dose reduction or cessation of treatment.
Lingjun Xu, Jing Wang, Gui-Dan Li, Kai-Feng Shen, Xing-Hui He, Wei Wu, Cuicui Liu   +6 more
semanticscholar   +1 more source

Nav1.7 inhibitors for the treatment of chronic pain

Bioorganic & Medicinal Chemistry Letters, 2018
The voltage gated sodium channel Nav1.7 plays an essential role in the transmission of pain signals. Strong human genetic validation has motivated extensive efforts to discover potent, selective, and efficacious Nav1.7 inhibitors for the treatment of chronic pain.
Steven J, McKerrall, Daniel P, Sutherlin
openaire   +2 more sources

ST‐2560, a selective inhibitor of the NaV1.7 sodium channel, affects nocifensive and cardiovascular reflexes in non‐human primates

British Journal of Pharmacology
The voltage‐gated sodium channel isoform NaV1.7 is a high‐interest target for the development of non‐opioid analgesics due to its preferential expression in pain‐sensing neurons.
John V Mulcahy, Jacob T. Beckley, Sheri Klas, Debra A Odink, A. Delwig, Hassan Pajouhesh, D. Monteleone, Xiang Zhou, J. Du Bois, David C Yeomans, George Luu, John C Hunter   +11 more
semanticscholar   +1 more source

A new Nav1.7 mutation in an erythromelalgia patient

Biochemical and Biophysical Research Communications, 2013
Gain-of-function missense mutations of SCN9A gene, which encodes voltage-gated sodium channel Nav1.7, alter channel's biophysical properties causing painful disorders which are refractory to pharmacotherapy in the vast majority of patients. Here we report a novel SCN9A mutation (ca.T3947C) in exon 20 in a 9 year old patient, not present in 200 ...
Mark, Estacion, Yang, Yang, Sulayman D, Dib-Hajj, Lynda, Tyrrell, Zhimiao, Lin, Yong, Yang, Stephen G, Waxman   +6 more
openaire   +2 more sources

Fenamates inhibit human sodium channel Nav1.7 and Nav1.8

Neuroscience Letters, 2019
Fenamates are N-substituted anthranilic acid derivatives, clinically used as nonsteroidal anti-inflammatory drugs (NSAIDs) in fever, pain and inflammation treatments. Previous studies have shown that they are also modulators of diverse ion channels, exhibiting either activation or inhibitory effects.
Jian-Fang, Sun, Yi-Jia, Xu, Xiao-Hua, Kong, Yang, Su, Zhan-You, Wang   +4 more
openaire   +2 more sources

Role of NaV1.7 in postganglionic sympathetic nerve function in human and guinea‐pig arteries

Journal of Physiology
NaV1.7 plays a crucial role in inducing and conducting action potentials in pain‐transducing sensory nociceptor fibres, suggesting that NaV1.7 blockers could be effective non‐opioid analgesics.
Joyce S. Kim, S. Meeker, Fei Ru, Minh Tran, Tanja S Zabka, David Hackos, B. Undem   +6 more
semanticscholar   +1 more source

Benzazepinone Nav1.7 blockers: Potential treatments for neuropathic pain

Bioorganic & Medicinal Chemistry Letters, 2007
A series of benzazepinones were synthesized and evaluated as hNa(v)1.7 sodium channel blockers. Several compounds from this series displayed good oral bioavailability and exposure and were efficacious in a rat model of neuropathic pain.
Scott B, Hoyt, Clare, London, Hyun, Ok, Edward, Gonzalez, Joseph L, Duffy, Catherine, Abbadie, Brian, Dean, John P, Felix, Maria L, Garcia, Nina, Jochnowitz, Bindhu V, Karanam, Xiaohua, Li, Kathryn A, Lyons, Erin, McGowan, D Euan, Macintyre, William J, Martin, Birgit T, Priest, McHardy M, Smith, Richard, Tschirret-Guth, Vivien A, Warren, Brande S, Williams, Gregory J, Kaczorowski, William H, Parsons   +22 more
openaire   +2 more sources

Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors

Bioorganic & Medicinal Chemistry Letters, 2018
Replacement of the piperidine ring in the lead benzenesulfonamide Nav1.7 inhibitor 1 with a weakly basic morpholine core resulted in a significant reduction in Nav1.7 inhibitory activity, but the activity was restored by shortening the linkage from methyleneoxy to oxygen.
Yong-Jin, Wu, Jason, Guernon, Andrea, McClure, Brian, Venables, Ramkumar, Rajamani, Kevin J, Robbins, Ronald J, Knox, Michele, Matchett, Rick L, Pieschl, James, Herrington, Linda J, Bristow, Nicholas A, Meanwell, Richard, Olson, Lorin A, Thompson, Carolyn, Dzierba   +14 more
openaire   +2 more sources

Nav1.7 Modulator Bearing a 3-Hydroxyindole Backbone Holds the Potential to Reverse Neuropathic Pain.

ACS Chemical Neuroscience
Chronic pain is a growing global health problem affecting at least 10% of the world's population. However, current chronic pain treatments are inadequate.
Yuwei Wang, Jirong Shu, Haoyi Yang, Kemiao Hong, Xiangji Yang, Weijie Guo, Jie Fang, Fuyi Li, Tao Liu, Zhiming Shan, Taoda Shi, Song Cai, Jian Zhang   +12 more
semanticscholar   +1 more source