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https://www.readbyqxmd.com/read/28440280/targeting-asic3-for-relieving-mice-fibromyalgia-pain-roles-of-electroacupuncture-opioid-and-adenosine
#1
Liang-Ta Yen, Ching-Liang Hsieh, Hsin-Cheng Hsu, Yi-Wen Lin
Many scientists are seeking better therapies for treating fibromyalgia (FM) pain. We used a mouse model of FM to determine if ASIC3 and its relevant signaling pathway participated in FM pain. We demonstrated that FM-induced mechanical hyperalgesia was attenuated by electroacupuncture (EA). The decrease in fatigue-induced lower motor function in FM mice was also reversed by EA. These EA-based effects were abolished by the opioid receptor antagonist naloxone and the adenosine A1 receptor antagonist rolofylline...
April 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28428547/the-tarantula-toxin-%C3%AE-%C3%AE-trtx-pre1a-highlights-the-importance-of-the-s1-s2-voltage-sensor-region-for-sodium-channel-subtype-selectivity
#2
Joshua S Wingerd, Christine A Mozar, Christine A Ussing, Swetha S Murali, Yanni K-Y Chin, Ben Cristofori-Armstrong, Thomas Durek, John Gilchrist, Christopher W Vaughan, Frank Bosmans, David J Adams, Richard J Lewis, Paul F Alewood, Mehdi Mobli, Macdonald J Christie, Lachlan D Rash
Voltage-gated sodium (NaV) channels are essential for the transmission of pain signals in humans making them prime targets for the development of new analgesics. Spider venoms are a rich source of peptide modulators useful to study ion channel structure and function. Here we describe β/δ-TRTX-Pre1a, a 35-residue tarantula peptide that selectively interacts with neuronal NaV channels inhibiting peak current of hNaV1.1, rNaV1.2, hNaV1.6, and hNaV1.7 while concurrently inhibiting fast inactivation of hNaV1.1 and rNaV1...
April 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28424991/expression-and-role-of-voltage-gated-sodium-channels-in-human-dorsal-root-ganglion-neurons-with-special-focus-on-nav1-7-species-differences-and-regulation-by-paclitaxel
#3
Wonseok Chang, Temugin Berta, Yong Ho Kim, Sanghoon Lee, Seok-Yong Lee, Ru-Rong Ji
Voltage-gated sodium channels (Navs) play an important role in human pain sensation. However, the expression and role of Nav subtypes in native human sensory neurons are unclear. To address this issue, we obtained human dorsal root ganglion (hDRG) tissues from healthy donors. PCR analysis of seven DRG-expressed Nav subtypes revealed that the hDRG has higher expression of Nav1.7 (~50% of total Nav expression) and lower expression of Nav1.8 (~12%), whereas the mouse DRG has higher expression of Nav1.8 (~45%) and lower expression of Nav1...
April 19, 2017: Neuroscience Bulletin
https://www.readbyqxmd.com/read/28420967/organization-and-plasticity-of-sodium-channel-expression-in-the-mouse-olfactory-and-vomeronasal-epithelia
#4
Florian Bolz, Stephanie Kasper, Bernd Bufe, Frank Zufall, Martina Pyrski
To understand the molecular basis of neuronal excitation in the mammalian olfactory system, we conducted a systematic analysis of the organization of voltage-gated sodium (Nav) channel subunits in the main olfactory epithelium (MOE) and vomeronasal organ (VNO) of adult mice. We also analyzed changes in Nav channel expression during development in these two systems and during regeneration of the MOE. Quantitative PCR shows that Nav1.7 is the predominant isoform in both adult MOE and VNO. We detected pronounced immunoreactivity for Nav1...
2017: Frontiers in Neuroanatomy
https://www.readbyqxmd.com/read/28412697/sema3a-signalling-requires-crmp1-and-nav1-7
#5
(no author information available yet)
No abstract text is available yet for this article.
April 15, 2017: Journal of Cell Science
https://www.readbyqxmd.com/read/28410768/-small-fiber-neuropathy
#6
V Langlois, A-L Bedat Millet, M Lebesnerais, S Miranda, F Marguet, Y Benhamou, P Marcorelles, H Lévesque
Small fiber neuropathy (SFN) is still unknown. Characterised by neuropathic pain, it typically begins by burning feet, but could take many other expression. SFN affects the thinly myelinated Aδ and unmyelinated C-fibers, by an inherited or acquired mechanism, which could lead to paresthesia, thermoalgic disorder or autonomic dysfunction. Recent studies suggest the preponderant role of ion channels such as Nav1.7. Furthermore, erythromelalgia or burning mouth syndrome are now recognized as real SFN. Various aetiologies of SFN are described...
April 11, 2017: La Revue de Médecine Interne
https://www.readbyqxmd.com/read/28389149/discovery-of-selective-orally-bioavailable-n-linked-arylsulfonamide-nav1-7-inhibitors-with-pain-efficacy-in-mice
#7
Anthony J Roecker, Melissa Egbertson, Kristen L G Jones, Robert Gomez, Richard L Kraus, Yuxing Li, Amy Jo Koser, Mark O Urban, Rebecca Klein, Michelle Clements, Jacqueline Panigel, Christopher Daley, Jixin Wang, Eleftheria N Finger, John Majercak, Vincent Santarelli, Irene Gregan, Matthew Cato, Tracey Filzen, Aneta Jovanovska, Ying-Hong Wang, Deping Wang, Leo A Joyce, Edward C Sherer, Xuanjia Peng, Xiu Wang, Haiyan Sun, Paul J Coleman, Andrea K Houghton, Mark E Layton
The voltage-gated sodium channel Nav1.7 is a genetically validated target for the treatment of pain with gain-of-function mutations in man eliciting a variety of painful disorders and loss-of-function mutations affording insensitivity to pain. Unfortunately, drugs thought to garner efficacy via Nav1 inhibition have undesirable side effect profiles due to their lack of selectivity over channel isoforms. Herein we report the discovery of a novel series of orally bioavailable arylsulfonamide Nav1.7 inhibitors with high levels of selectivity over Nav1...
March 30, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28381558/gain-of-function-mutation-of-a-voltage-gated-sodium-channel-nav1-7-associated-with-peripheral-pain-and-impaired-limb-development
#8
Brian S Tanaka, Phuong T Nguyen, Eray Yihui Zhou, Yong Yang, Vladimir Yarov-Yarovoy, Sulayman D Dib-Hajj, Stephen G Waxman
Dominant mutations in voltage-gated sodium channel NaV1.7 cause inherited erythromelalgia (IEM), a debilitating pain disorder characterized by severe burning pain and redness of the distal extremities. NaV1.7 is preferentially expressed within peripheral sensory and sympathetic neurons. Here, we describe a novel NaV1.7 mutation in an 11-year old male with under-development of the limbs, recurrent attacks of burning pain with erythema and swelling in his feet and hands. Frequency and duration of the episodes gradually increased with age and relief by cooling became less effective...
April 5, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28375911/trigeminal-neuralgia
#9
Giorgio Cruccu
PURPOSE OF REVIEW: Although trigeminal neuralgia is well known to neurologists, recent developments in classification and clinical diagnosis, new MRI methods, and a debate about surgical options necessitate an update on the topic. RECENT FINDINGS: Currently, a worldwide controversy exists regarding the classification, diagnostic process, and surgical treatment of trigeminal neuralgia. This controversy has been caused on one side by the recognition that some 50% of patients with trigeminal neuralgia, apart from characteristic paroxysmal attacks, also have continuous pain in the same territory, which results in greater diagnostic difficulties and is associated with a lower response to medical and surgical treatments...
April 2017: Continuum: Lifelong Learning in Neurology
https://www.readbyqxmd.com/read/28349234/prostaglandin-e2-upregulated-trigeminal-ganglionic-sodium-channel-1-7-involving-temporomandibular-joint-inflammatory-pain-in-rats
#10
Peng Zhang, Ye-Hua Gan
Prostaglandin E2 (PGE2) is a key proinflammatory mediator that contributes to inflammatory hyperalgesia. Voltage-gated sodium channel 1.7 (Nav1.7) plays an important role in inflammatory pain. However, the modulation of Nav1.7 in inflammatory pain remains poorly understood. We hypothesized that PGE2 might regulate Nav1.7 expression in inflammatory pain. We here showed that treatment of rat trigeminal ganglion (TG) explants with PGE2 significantly upregulated the mRNA and protein expressions of Nav1.7 through PGE2 receptor EP2...
March 27, 2017: Inflammation
https://www.readbyqxmd.com/read/28337335/correction-to-sulfonamides-as-selective-nav1-7-inhibitors-optimizing-potency-and-pharmacokinetics-to-enable-in-vivo-target-engagement
#11
Isaac E Marx, Thomas A Dineen, Jessica Able, Christiane Bode, Howard Bregman, Margaret Chu-Moyer, Erin F DiMauro, Bingfan Du, Robert S Foti, Robert T Fremeau, Hua Gao, Hakan Gunaydin, Brian E Hall, Liyue Huang, Thomas Kornecook, Charles R Kreiman, Daniel S La, Joseph Ligutti, Min-Hwa Jasmine Lin, Dong Liu, Jeff S McDermott, Bryan D Moyer, Hanh N Nguyen, Emily A Peterson, Jonathan T Roberts, Paul Rose, Jean Wang, Beth D Youngblood, Violeta Yu, Matthew M Weiss
[This corrects the article DOI: 10.1021/acsmedchemlett.6b00243.].
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28324649/sulfonamides-as-selective-nav1-7-inhibitors-optimizing-potency-pharmacokinetics-and-metabolic-properties-to-obtain-atropisomeric-quinolinone-am-0466-that-affords-robust-in-vivo-activity
#12
Russell F Graceffa, Alessandro A Boezio, Jessica Able, Steven Altmann, Loren M Berry, Christiane Boezio, John R Butler, Margaret Chu-Moyer, Melanie Cooke, Erin F DiMauro, Thomas A Dineen, Elma Feric Bojic, Robert S Foti, Robert T Fremeau, Angel Guzman-Perez, Hua Gao, Hakan Gunaydin, Hongbing Huang, Liyue Huang, Christopher Ilch, Michael Jarosh, Thomas Kornecook, Charles R Kreiman, Daniel S La, Joseph Ligutti, Benjamin C Milgram, Min-Hwa Jasmine Lin, Isaac E Marx, Hanh N Nguyen, Emily A Peterson, Gwen Rescourio, John Roberts, Laurie Schenkel, Roman Shimanovich, Brian A Sparling, John Stellwagen, Kristin Taborn, Karina R Vaida, Jean Wang, John Yeoman, Violeta Yu, Dawn Zhu, Bryan D Moyer, Matthew M Weiss
Because of its strong genetic validation, NaV1.7 has attracted significant interest as a target for the treatment of pain. We have previously reported on a number of structurally distinct bicyclic heteroarylsulfonamides as NaV1.7 inhibitors that demonstrate high levels of selectivity over other NaV isoforms. Herein, we report the discovery and optimization of a series of atropisomeric quinolinone sulfonamide inhibitors [ Bicyclic sulfonamide compounds as sodium channel inhibitors and their preparation . WO 2014201206, 2014 ] of NaV1...
April 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28301520/the-structure-dynamics-and-selectivity-profile-of-a-nav1-7-potency-optimised-huwentoxin-iv-variant
#13
Sassan Rahnama, Jennifer R Deuis, Fernanda C Cardoso, Venkatraman Ramanujam, Richard J Lewis, Lachlan D Rash, Glenn F King, Irina Vetter, Mehdi Mobli
Venom-derived peptides have attracted much attention as potential lead molecules for pharmaceutical development. A well-known example is Huwentoxin-IV (HwTx-IV), a peptide toxin isolated from the venom of the Chinese bird-eating spider Haplopelma schmitdi. HwTx-IV was identified as a potent blocker of a human voltage-gated sodium channel (hNaV1.7), which is a genetically validated analgesic target. The peptide was promising as it showed high potency at NaV1.7 (IC50 ~26 nM) and selectivity over the cardiac NaV subtype (NaV1...
2017: PloS One
https://www.readbyqxmd.com/read/28287723/sulfonamides-as-selective-nav1-7-inhibitors-optimizing-potency-and-pharmacokinetics-while-mitigating-metabolic-liabilities
#14
Matthew M Weiss, Thomas A Dineen, Isaac E Marx, Steven Altmann, Alessandro Boezio, Howard Bregman, Margaret Chu-Moyer, Erin F DiMauro, Elma Feric Bojic, Robert S Foti, Hua Gao, Russell Graceffa, Hakan Gunaydin, Angel Guzman-Perez, Hongbing Huang, Liyue Huang, Michael Jarosh, Thomas Kornecook, Charles R Kreiman, Joseph Ligutti, Daniel S La, Min-Hwa Jasmine Lin, Dong Liu, Bryan D Moyer, Hanh N Nguyen, Emily A Peterson, Paul E Rose, Kristin Taborn, Beth D Youngblood, Violeta Yu, Robert T Fremeau
Several reports have recently emerged regarding the identification of heteroarylsulfonamides as NaV1.7 inhibitors that demonstrate high levels of selectivity over other NaV isoforms. The optimization of a series of internal NaV1.7 leads that address a number of metabolic liabilities including bioactivation, PXR activation, as well as CYP3A4 induction and inhibition led to the identification of potent and selective inhibitors that demonstrated favorable pharmacokinetic profiles and were devoid of the aforementioned liabilities...
April 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28277940/a-single-structurally-conserved-sumoylation-site-in-crmp2-controls-nav1-7-function
#15
Erik Thomas Dustrude, Samantha Perez-Miller, Liberty François-Moutal, Aubin Moutal, May Khanna, Rajesh Khanna
The neuronal collapsin response mediator protein 2 (CRMP2) undergoes several posttranslational modifications that codify its functions. Most recently, CRMP2 SUMOylation (addition of small ubiquitin like modifier (SUMO)) was identified as a key regulatory step within a modification program that codes for CRMP2 interaction with, and trafficking of, voltage-gated sodium channel NaV1.7. In this paper, we illustrate the utility of combining sequence alignment within protein families with structural analysis to identify, from several putative SUMOylation sites, those that are most likely to be biologically relevant...
February 28, 2017: Channels
https://www.readbyqxmd.com/read/28266963/safety-and-efficacy-of-a-topical-sodium-channel-inhibitor-tv-45070-in-patients-with-postherpetic-neuralgia-phn-a-randomized-controlled-proof-of-concept-crossover-study-with-a-subgroup-analysis-of-the-nav1-7-r1150w-genotype
#16
Nicola Price, Rostam Namdari, Judith Neville, Katie J W Proctor, Samer Kaber, Jeffery Vest, Michael Fetell, Richard Malamut, Robin P Sherrington, Simon N Pimstone, Yigal P Goldberg
OBJECTIVE: The objective was to evaluate the safety and efficacy of TV-45070 ointment, as a treatment for postherpetic neuralgia, and to explore the response in patients with the Nav1.7 R1150W gain-of-function polymorphism. MATERIALS AND METHODS: This was a randomized, placebo-controlled, 2-period, 2-treatment crossover trial. Patients with postherpetic neuralgia with moderate or greater pain received TV-45070 and placebo ointments, each applied twice daily for 3 weeks...
April 2017: Clinical Journal of Pain
https://www.readbyqxmd.com/read/28254884/a-functional-coupling-between-crmp1-and-nav1-7-for-retrograde-propagation-of-semaphorin3a-signaling
#17
Masayuki Yamane, Naoya Yamashita, Tomonobu Hida, Yoshinori Kamiya, Fumio Nakamura, Pappachan Kolattukudy, Yoshio Goshima
Semaphorin3A (Sema3A) is a secreted type of axon guidance molecule that regulates axon wiring through complexes of neuropilin-1 (NRP1) with PlexinA protein receptors. Sema3A regulates the dendritic branching through tetrodotoxin (TTX)-sensitive retrograde axonal transport of PlexA proteins and tropomyosin-related kinase A (TrkA) complex. We here demonstrate that Nav1.7 (encoded by SCN9A), a TTX-sensitive Na(+) channel, by coupling with collapsin response mediator protein 1 (CRMP1), mediates the Sema3A-induced retrograde transport...
April 15, 2017: Journal of Cell Science
https://www.readbyqxmd.com/read/28243733/biophysical-and-molecular-comparison-of-sodium-current-in-cells-isolated-from-canine-atria-and-pulmonary-vein
#18
Hector Barajas-Martinez, Robert J Goodrow, Dan Hu, Payal Patel, Mayurika Desai, Brian K Panama, Jacqueline A Treat, Gary L Aistrup, Jonathan M Cordeiro
The collar of the pulmonary vein (PV) is the focal point for the initiation of atrial arrhythmias, but the mechanisms underlying how PV cells differ from neighboring left atrial tissue are unclear. We examined the biophysical and molecular properties of INa in cells isolated from the canine pulmonary sleeve and compared the properties to left atrial tissue. PV and left atrial myocytes were isolated and patch clamp techniques were used to record INa. Action potential recordings from either tissue type were made using high-resistance electrodes...
February 27, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28235406/network-topology-of-nav1-7-mutations-in-sodium-channel-related-painful-disorders
#19
Dimos Kapetis, Jenny Sassone, Yang Yang, Barbara Galbardi, Markos N Xenakis, Ronald L Westra, Radek Szklarczyk, Patrick Lindsey, Catharina G Faber, Monique Gerrits, Ingemar S J Merkies, Sulayman D Dib-Hajj, Massimo Mantegazza, Stephen G Waxman, Giuseppe Lauria
BACKGROUND: Gain-of-function mutations in SCN9A gene that encodes the voltage-gated sodium channel NaV1.7 have been associated with a wide spectrum of painful syndromes in humans including inherited erythromelalgia, paroxysmal extreme pain disorder and small fibre neuropathy. These mutations change the biophysical properties of NaV1.7 channels leading to hyperexcitability of dorsal root ganglion nociceptors and pain symptoms. There is a need for better understanding of how gain-of-function mutations alter the atomic structure of Nav1...
February 24, 2017: BMC Systems Biology
https://www.readbyqxmd.com/read/28225079/multiple-sodium-channel-isoforms-mediate-the-pathological-effects-of-pacific-ciguatoxin-1
#20
Marco C Inserra, Mathilde R Israel, Ashlee Caldwell, Joel Castro, Jennifer R Deuis, Andrea M Harrington, Angelo Keramidas, Sonia Garcia-Caraballo, Jessica Maddern, Andelain Erickson, Luke Grundy, Grigori Y Rychkov, Katharina Zimmermann, Richard J Lewis, Stuart M Brierley, Irina Vetter
Human intoxication with the seafood poison ciguatoxin, a dinoflagellate polyether that activates voltage-gated sodium channels (NaV), causes ciguatera, a disease characterised by gastrointestinal and neurological disturbances. We assessed the activity of the most potent congener, Pacific ciguatoxin-1 (P-CTX-1), on NaV1.1-1.9 using imaging and electrophysiological approaches. Although P-CTX-1 is essentially a non-selective NaV toxin and shifted the voltage-dependence of activation to more hyperpolarising potentials at all NaV subtypes, an increase in the inactivation time constant was observed only at NaV1...
February 22, 2017: Scientific Reports
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