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https://www.readbyqxmd.com/read/28522215/blocking-voltage-gated-sodium-channels-as-a-strategy-to-suppress-pathological-cough
#1
REVIEW
Hui Sun, Marian Kollarik, Bradley J Undem
Pathological cough is thought to be secondary to inappropriate activation of vagal sensory nerves. Sensory nerves can be activated by a large number of disparate stimuli. The most relevant stimuli to block for effective anti-tussive therapy likely depend on the specific underlying pathology that is leading to the coughing. Blocking voltage-gated sodium channels (NaV) will prevent action potential initiation and conduction and therefore prevent sensory communication between the airways and brainstem. In so doing, they would be expected to inhibit evoked cough independently of the nature of the stimulus and underlying pathology...
May 15, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28473457/pharmacologic-characterization-of-amg8379-a-potent-and-selective-small-molecule-sulfonamide-antagonist-of-the-voltage-gated-sodium-channel-nav1-7
#2
Thomas J Kornecook, Ruoyuan Yin, Stephen Altmann, Xuhai Be, Virginia Berry, Christopher P Ilch, Michael Jarosh, Danielle Johnson, Josie H Lee, Sonya G Lehto, Joseph Ligutti, Dong Liu, Jason Luther, David Matson, Danny Ortuno, John Roberts, Kristin Taborn, Jinti Wang, Matthew M Weiss, Violeta Yu, Dawn X D Zhu, Robert T Fremeau, Bryan D Moyer
Potent and selective antagonists of the voltage-gated sodium channel NaV1.7 represent a promising avenue for the development of new chronic pain therapies. We generated a small molecule atropisomer quinolone sulfonamide antagonist AMG8379 and a less active enantiomer AMG8380. Here we show that AMG8379 potently blocks human NaV1.7 channels with an IC50 of 8.5 nM and endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM in whole cell patch clamp electrophysiology assays using a voltage protocol that interrogates channels in a partially inactivated state...
May 4, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28450535/sodium-channel-nav1-8-underlies-ttx-resistant-axonal-action-potential-conduction-in-somatosensory-c-fibers-of-distal-cutaneous-nerves
#3
A H Klein, A Vyshnevska, T V Hartke, R De Col, J L Mankowski, B P Turnquist, F Bosmans, P W Reeh, M Schmelz, R W Carr, M Ringkamp
Voltage gated sodium (NaV) channels are responsible for the initiation and conduction of action potentials within primary afferents. The nine NaV isoforms recognized in mammals are often functionally divided into tetrodotoxin (TTX)-sensitive(s) channels (NaV1.1-NaV1.4, NaV1.6-NaV1.7) that are blocked by nanomolar concentrations and TTX-resistant(r) channels (NaV1.8 and NaV1.9) inhibited by millimolar concentrations with NaV1.5 having an intermediate toxin sensitivity. For small diameter primary afferent neurons, it is unclear to what extent different NaV channel isoforms are distributed along the peripheral and central branches of their bifurcated axons...
April 27, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28425222/class-iii-antiarrhythmic-drugs-amiodarone-and-dronedarone-impair-kir-2-1-backward-trafficking
#4
Yuan Ji, Hiroki Takanari, Muge Qile, Lukas Nalos, Marien J C Houtman, Fee L Romunde, Raimond Heukers, Paul M P van Bergen En Henegouwen, Marc A Vos, Marcel A G van der Heyden
Drug-induced ion channel trafficking disturbance can cause cardiac arrhythmias. The subcellular level at which drugs interfere in trafficking pathways is largely unknown. KIR 2.1 inward rectifier channels, largely responsible for the cardiac inward rectifier current (IK1 ), are degraded in lysosomes. Amiodarone and dronedarone are class III antiarrhythmics. Chronic use of amiodarone, and to a lesser extent dronedarone, causes serious adverse effects to several organs and tissue types, including the heart. Both drugs have been described to interfere in the late-endosome/lysosome system...
April 19, 2017: Journal of Cellular and Molecular Medicine
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
#5
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/28418213/pain-thresholds-supra-threshold-pain-and-lidocaine-sensitivity-in-patients-with-erythromelalgia-including-the-i848tmutation-in-nav-1-7
#6
T Helås, D Sagafos, I P Kleggetveit, H Quiding, B Jönsson, M Segerdahl, Z Zhang, H Salter, M Schmelz, E Jørum
OBJECTIVES: Nociceptive thresholds and supra-threshold pain ratings as well as their reduction upon local injection with lidocaine were compared between healthy subjects and patients with erythromelalgia (EM). METHODS: Lidocaine (0.25, 0.50, 1.0 or 10 mg/mL) or placebo (saline) was injected intradermally in non-painful areas of the lower arm, in a randomized, double-blind manner, to test the effect on dynamic and static mechanical sensitivity, mechanical pain sensitivity, thermal thresholds and supra-threshold heat pain sensitivity...
April 18, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28380690/chemogenetic-inhibition-of-pain-neurons-in-a-mouse-model-of-osteoarthritis
#7
Rachel E Miller, Shingo Ishihara, Bula Bhattacharyya, Ada Delaney, Daniela M Menichella, Richard J Miller, Anne-Marie Malfait
Objective - The purpose of this study was to determine the ability of drugs that activate inhibitory G-protein coupled receptors (GPCRs) expressed in peripheral NaV 1.8-positive sensory neurons to control osteoarthritis associated pain. Therefore, we used Designer Receptors Exclusively Activated by a Designer Drug (DREADD) technology, which utilizes engineered GPCRs to activate or inhibit neurons upon binding the synthetic ligand, clozapine-N-oxide. Methods -NaV 1.8-Pdi C57BL/6 mice were created to express the inhibitory DREADD receptor, Pdi, in NaV 1...
April 5, 2017: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/28296957/computer-assisted-electromagnetic-navigation-improves-accuracy-in-computed-tomography-guided-interventions-a-prospective-randomized-clinical-trial
#8
Pierre Durand, Alexandre Moreau-Gaudry, Anne-Sophie Silvent, Julien Frandon, Emilie Chipon, Maud Médici, Ivan Bricault
PURPOSE: To assess the accuracy and usability of an electromagnetic navigation system designed to assist Computed Tomography (CT) guided interventions. MATERIALS AND METHODS: 120 patients requiring a percutaneous CT intervention (drainage, biopsy, tumor ablation, infiltration, sympathicolysis) were included in this prospective randomized trial. Nineteen radiologists participated. Conventional procedures (CT group) were compared with procedures assisted by a navigation system prototype using an electromagnetic localizer to track the position and orientation of a needle holder (NAV group)...
2017: PloS One
https://www.readbyqxmd.com/read/28225079/multiple-sodium-channel-isoforms-mediate-the-pathological-effects-of-pacific-ciguatoxin-1
#9
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
https://www.readbyqxmd.com/read/28216001/loperamide-inhibits-sodium-channels-to-alleviate-inflammatory-hyperalgesia
#10
Ying Wu, Beiyan Zou, Lingli Liang, Min Li, Yuan-Xiang Tao, Haibo Yu, Xiaoliang Wang, Min Li
Previous studies demonstrated that Loperamide, originally known as an anti-diarrheal drug, is a promising analgesic agent primarily targeting mu-opioid receptors. However some evidences suggested that non-opioid mechanisms may be contributing to its analgesic effect. In the present study, Loperamide was identified as a Nav1.7 blocker in a pilot screen. In HEK293 cells expressing Nav1.7 sodium channels, Loperamide blocked the resting state of Nav1.7 channels (IC50 = 1.86 ± 0.11 μM) dose-dependently and reversibly...
February 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28166971/functional-and-molecular-characterization-of-voltage-gated-sodium-channel-nav-1-8-in-bull-spermatozoa
#11
Dharmendra Singh Chauhan, Dilip Kumar Swain, Nadeem Shah, Hanuman Prasad Yadav, Udayraj P Nakade, Vijay Kumar Singh, Rajesh Nigam, Sarvajeet Yadav, Satish Kumar Garg
The aim of our study was to characterize the voltage gated sodium channel Nav 1.8 in bull spermatozoa. Forty ejaculates were collected from four Hariana bulls and semen samples were pooled in view of the nonsignificant variations between different ejaculates. Functional characterization was undertaken using A-803467, a selective blocker of Nav1.8, and veratridine as an opener of the voltage gated sodium channels while molecular characterization was done using western blotting and indirect immunofluorescence assays...
March 1, 2017: Theriogenology
https://www.readbyqxmd.com/read/28105664/visceral-and-somatic-pain-modalities-reveal-nav-1-7-independent-visceral-nociceptive-pathways
#12
James R F Hockley, Rafael González-Cano, Sheridan McMurray, Miguel A Tejada-Giraldez, Cian McGuire, Antonio Torres, Anna L Wilbrey, Vincent Cibert-Goton, Francisco R Nieto, Thomas Pitcher, Charles H Knowles, José Manuel Baeyens, John N Wood, Wendy J Winchester, David C Bulmer, Cruz Miguel Cendán, Gordon McMurray
KEY POINTS: Voltage-gated sodium channels play a fundamental role in determining neuronal excitability. Specifically, voltage-gated sodium channel subtype NaV 1.7 is required for sensing acute and inflammatory somatic pain in mice and humans but its significance in pain originating from the viscera is unknown. Using comparative behavioural models evoking somatic and visceral pain pathways, we identify the requirement for NaV 1.7 in regulating somatic (noxious heat pain threshold) but not in visceral pain signalling...
April 15, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/27903401/-impact-of-neuronal-sodium-channel-nav-1-8-on-cardiac-function-and-cardiovascular-diseases
#13
(no author information available yet)
No abstract text is available yet for this article.
November 24, 2016: Zhonghua Xin Xue Guan Bing za Zhi
https://www.readbyqxmd.com/read/27896032/gene-expression-profile-of-sodium-channel-subunits-in-the-anterior-cingulate-cortex-during-experimental-paclitaxel-induced-neuropathic-pain-in-mice
#14
Willias Masocha
Paclitaxel, a chemotherapeutic agent, causes neuropathic pain whose supraspinal pathophysiology is not fully understood. Dysregulation of sodium channel expression, studied mainly in the periphery and spinal cord level, contributes to the pathogenesis of neuropathic pain. We examined gene expression of sodium channel (Nav) subunits by real time polymerase chain reaction (PCR) in the anterior cingulate cortex (ACC) at day 7 post first administration of paclitaxel, when mice had developed paclitaxel-induced thermal hyperalgesia...
2016: PeerJ
https://www.readbyqxmd.com/read/27679933/controlled-banked-turns-in-coleopteran-flight-measured-by-a-miniature-wireless-inertial-measurement-unit
#15
Yao Li, Feng Cao, Tat Thang Vo Doan, Hirotaka Sato
The mechanisms and principles of insect flight have long been investigated by researchers working on micro and nano air vehicles (MAVs/NAVs). However, studies of insect flight maneuvers require high speed filming and high spatial resolution in a small experimental space, or the tethering of the insect to a fixed place. Under such artificial conditions, the insects may deviate its flying behavior from that of regular flight. In this study, we mounted a tiny wireless system, or 'backpack', on live beetles (Mecynorrhina torquata; length 62 ± 8 mm; mass 7...
2016: Bioinspiration & Biomimetics
https://www.readbyqxmd.com/read/27324898/protein-profile-and-morphological-alterations-in-penumbra-after-focal-photothrombotic-infarction-in-the-rat-cerebral-cortex
#16
Anatoly Uzdensky, Svetlana Demyanenko, Grigory Fedorenko, Tayana Lapteva, Alexej Fedorenko
After ischemic stroke, cell damage propagates from infarct core to surrounding tissues (penumbra). To reveal proteins involved in neurodegeneration and neuroprotection in penumbra, we studied protein expression changes in 2-mm ring around the core of photothrombotic infarct induced in the rat brain cortex by local laser irradiation after administration of Bengal Rose. The ultrastructural study showed edema and degeneration of neurons, glia, and capillaries. Morphological changes gradually decreased across the penumbra...
June 21, 2016: Molecular Neurobiology
https://www.readbyqxmd.com/read/27272739/association-of-common-and-rare-variants-of-scn10a-gene-with-sudden-unexplained-nocturnal-death-syndrome-in-chinese-han-population
#17
Liyong Zhang, Feng Zhou, Lei Huang, Qiuping Wu, Jinxiang Zheng, Yeda Wu, Kun Yin, Jianding Cheng
Sudden unexplained nocturnal death syndrome (SUNDS) remains an autopsy negative entity with unknown etiology to both forensic pathologists and physicians. The electrocardiogram (ECG) characteristics and clinical phenotype of SUNDS survivors strongly suggest that SUNDS shares some similarities with Brugada syndrome (BrS). Recently, the variants of sodium channel Nav 1.8 coding gene SCN10A were identified to be associated with BrS. Here, we investigated the association of SCN10A gene variants with 105 sporadic SUNDS victims and 22 BrS cases in the Chinese Han population...
January 2017: International Journal of Legal Medicine
https://www.readbyqxmd.com/read/27271997/t-boc-synthesis-of-huwentoxin-i-through-native-chemical-ligation-incorporating-a-trifluoromethanesulfonic-acid-cleavage-strategy
#18
Parashar Thapa, Chino C Cabalteja, Edwin E Philips, Michael J Espiritu, Steve Peigneur, Bea G Mille, Jan Tytgat, Theodore R Cummins, Jon-Paul Bingham
Tert-butyloxycarbonyl (t-Boc)-based native chemical ligation (NCL) techniques commonly employ hydrogen fluoride (HF) to create the thioester fragment required for the ligation process. Our research aimed to assess the replacement of HF with Trifluoromethanesulfonic acid (TFMSA). Here we examined a 33 amino acid test peptide, Huwentoxin-I (HwTx-I) as a novel candidate for our TFMSA cleavage protocol. Structurally HwTx-I has an X-Cys(16) -Cys(17) -X sequence mid-region, which makes it an ideal candidate for NCL...
September 2016: Biopolymers
https://www.readbyqxmd.com/read/27187983/safety-and-effectiveness-of-the-nav-6-filter-in-preventing-distal-embolization-during-jetstream-atherectomy-of-infrainguinal-peripheral-artery-lesions
#19
Avantika Banerjee, Karan Sarode, Atif Mohammad, Emmanouil S Brilakis, Subhash Banerjee, Gail A Shammas, Nicolas W Shammas
BACKGROUND: The risk of distal embolization (DE) during infrainguinal peripheral artery interventions (PAI) is often mitigated by the use of embolic protection devices. There are limited data on the use of filters with the Jetstream (JS) atherectomy device, a rotational cutter with aspiration capacity. The Nav-6 filter is uniquely suited for use with the JS due to its wire compatibility and detachment from the filter; however, data on the off-label use of this combination have not been reported...
August 2016: Journal of Invasive Cardiology
https://www.readbyqxmd.com/read/27130441/differential-inhibition-of-cardiac-and-neuronal-na-channels-by-the-selective-serotonin-norepinephrine-reuptake-inhibitors-duloxetine-and-venlafaxine
#20
Carsten Stoetzer, Bastian Papenberg, Thorben Doll, Marc Völker, Joerg Heineke, Marcus Stoetzer, Florian Wegner, Andreas Leffler
Duloxetine and venlafaxine are selective serotonin-norepinephrine-reuptake-inhibitors used as antidepressants and co-analgesics. While venlafaxine rather than duloxetine induce cardiovascular side-effects, neither of the substances are regarded cardiotoxic. Inhibition of cardiac Na(+)-channels can be associated with cardiotoxicity, and duloxetine was demonstrated to block neuronal Na(+)-channels. The aim of this study was to investigate if the non-life threatening cardiotoxicities of duloxetine and venlafaxine correlate with a weak inhibition of cardiac Na(+)-channels...
July 15, 2016: European Journal of Pharmacology
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