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https://www.readbyqxmd.com/read/29783906/bulleyaconitine-a-attenuates-hyperexcitability-of-dorsal-root-ganglion-neurons-induced-by-spared-nerve-injury-the-role-of-preferably-blocking-nav1-7-and-nav1-3-channels
#1
Man-Xiu Xie, Jie Yang, Rui-Ping Pang, Wei-An Zeng, Han-Dong Ouyang, Yan-Qing Liu, Xian-Guo Liu
Background Oral administration of Bulleyaconitine A, an extracted diterpenoid alkaloid from Aconitum bulleyanum plants, is effective for treating chronic pain in rats and in human patients, but the underlying mechanisms are poorly understood. Results As the hyperexcitability of dorsal root ganglion neurons resulting from the upregulation of voltage-gated sodium (Nav) channels has been proved critical for development of chronic pain, we tested the effects of Bulleyaconitine A on Nav channels in rat spared nerve injury model of neuropathic pain...
January 2018: Molecular Pain
https://www.readbyqxmd.com/read/29769724/structural-basis-for-gating-pore-current-in-periodic-paralysis
#2
Daohua Jiang, Tamer M Gamal El-Din, Christopher Ing, Peilong Lu, Régis Pomès, Ning Zheng, William A Catterall
Potassium-sensitive hypokalaemic and normokalaemic periodic paralysis are inherited skeletal muscle diseases characterized by episodes of flaccid muscle weakness1,2 . They are caused by single mutations in positively charged residues ('gating charges') in the S4 transmembrane segment of the voltage sensor of the voltage-gated sodium channel Nav 1.4 or the calcium channel Cav 1.11,2 . Mutations of the outermost gating charges (R1 and R2) cause hypokalaemic periodic paralysis1,2 by creating a pathogenic gating pore in the voltage sensor through which cations leak in the resting state3,4 ...
May 16, 2018: Nature
https://www.readbyqxmd.com/read/29735899/determination-of-the-%C3%AE-conotoxin-piiia-specificity-against-voltage-gated-sodium-channels-from-binding-energy-calculations
#3
Fangling Chen, Wenxin Huang, Tao Jiang, Rilei Yu
Voltage-gated sodium (NaV ) channels generate and propagate action potentials in excitable cells, and several NaV subtypes have become important targets for pain management. The μ-conotoxins inhibit subtypes of the NaV with varied specificity but often lack of specificity to interested subtypes. Engineering the selectivity of the μ-conotoxins presents considerable complexity and challenge, as it involves the optimization of their binding affinities to multiple highly conserved NaV subtypes. In this study, a model of NaV 1...
May 7, 2018: Marine Drugs
https://www.readbyqxmd.com/read/29686617/a-chimeric-nav1-8-channel-expression-system-based-on-hek293t-cell-line
#4
Xi Zhou, Yunxiao Zhang, Dongfang Tang, Songping Liang, Ping Chen, Cheng Tang, Zhonghua Liu
Among the nine voltage-gated sodium channel (NaV) subtypes, NaV1.8 is an attractive therapeutic target for pain. The heterologous expression of recombinant NaV1.8 currents is of particular importance for its electrophysiological and pharmacological studies. However, NaV1.8 expresses no or low-level functional currents when transiently transfected into non-neuronal cell lines. The present study aims to explore the molecular determinants limiting its functional expression and accordingly establish a functional NaV1...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29673577/profiling-of-g-protein-coupled-receptors-in-vagal-afferents-reveals-novel-gut-to-brain-sensing-mechanisms
#5
Kristoffer L Egerod, Natalia Petersen, Pascal N Timshel, Jens C Rekling, Yibing Wang, Qinghua Liu, Thue W Schwartz, Laurent Gautron
OBJECTIVES: G protein-coupled receptors (GPCRs) act as transmembrane molecular sensors of neurotransmitters, hormones, nutrients, and metabolites. Because unmyelinated vagal afferents richly innervate the gastrointestinal mucosa, gut-derived molecules may directly modulate the activity of vagal afferents through GPCRs. However, the types of GPCRs expressed in vagal afferents are largely unknown. Here, we determined the expression profile of all GPCRs expressed in vagal afferents of the mouse, with a special emphasis on those innervating the gastrointestinal tract...
April 3, 2018: Molecular Metabolism
https://www.readbyqxmd.com/read/29559913/novel-sodium-channel-inhibitor-from-leeches
#6
Gan Wang, Chengbo Long, Weihui Liu, Cheng Xu, Min Zhang, Qiong Li, Qiumin Lu, Ping Meng, Dongsheng Li, Mingqiang Rong, Zhaohui Sun, Xiaodong Luo, Ren Lai
Considering blood-sucking habits of leeches from surviving strategy of view, it can be hypothesized that leech saliva has analgesia or anesthesia functions for leeches to stay undetected by the host. However, no specific substance with analgesic function has been reported from leech saliva although clinical applications strongly indicated that leech therapy produces a strong and long lasting pain-reducing effect. Herein, a novel family of small peptides (HSTXs) including 11 members which show low similarity with known peptides was identified from salivary glands of the leech Haemadipsa sylvestris ...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29554219/prrt2-controls-neuronal-excitability-by-negatively-modulating-na-channel-1-2-1-6-activity
#7
Floriana Fruscione, Pierluigi Valente, Bruno Sterlini, Alessandra Romei, Simona Baldassari, Manuela Fadda, Cosimo Prestigio, Giorgia Giansante, Jacopo Sartorelli, Pia Rossi, Alicia Rubio, Antonio Gambardella, Thierry Nieus, Vania Broccoli, Anna Fassio, Pietro Baldelli, Anna Corradi, Federico Zara, Fabio Benfenati
Proline-rich transmembrane protein 2 (PRRT2) is the causative gene for a heterogeneous group of familial paroxysmal neurological disorders that include seizures with onset in the first year of life (benign familial infantile seizures), paroxysmal kinesigenic dyskinesia or a combination of both. Most of the PRRT2 mutations are loss-of-function leading to haploinsufficiency and 80% of the patients carry the same frameshift mutation (c.649dupC; p.Arg217Profs*8), which leads to a premature stop codon. To model the disease and dissect the physiological role of PRRT2, we studied the phenotype of neurons differentiated from induced pluripotent stem cells from previously described heterozygous and homozygous siblings carrying the c...
March 15, 2018: Brain: a Journal of Neurology
https://www.readbyqxmd.com/read/29501398/the-peptide-toxin-%C3%AE-hexatoxin-mrix-inhibits-fast-inactivation-of-na-v-s-in-mouse-cerebellar-granule-cells
#8
Dongfang Tang, Zhen Xiao, Yan Xu, Jiao Zeng, Dezheng Peng, Songping Liang, Cheng Tang, Zhonghua Liu
Spider venom is rich in peptide toxins that could be used to explore the structure and function of voltage-gated sodium channels (NaV s). This study has characterized a 44-amino acid peptide toxin, δ-hexatoxin-MrIX (δ-HXTX-MrIX), from the venom of the spider Macrothele raveni. δ-hexatoxin-MrIX potently inhibited the fast inactivation of NaV s in mouse cerebellar granule cells (CGCs) with an EC50 of 35.3 ± 5.9 nM. The toxin shifted both the steady-state activation and the steady-state inactivation curves of CGC NaV s to the hyperpolarized direction...
April 2018: Peptides
https://www.readbyqxmd.com/read/29497094/conditional-knockout-of-na-v-1-6-in-adult-mice-ameliorates-neuropathic-pain
#9
Lubin Chen, Jianying Huang, Peng Zhao, Anna-Karin Persson, Fadia B Dib-Hajj, Xiaoyang Cheng, Andrew Tan, Stephen G Waxman, Sulayman D Dib-Hajj
Voltage-gated sodium channels NaV 1.7, NaV 1.8 and NaV 1.9 have been the focus for pain studies because their mutations are associated with human pain disorders, but the role of NaV 1.6 in pain is less understood. In this study, we selectively knocked out NaV 1.6 in dorsal root ganglion (DRG) neurons, using NaV 1.8-Cre directed or adeno-associated virus (AAV)-Cre mediated approaches, and examined the specific contribution of NaV 1.6 to the tetrodotoxin-sensitive (TTX-S) current in these neurons and its role in neuropathic pain...
March 1, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29496495/assessment-of-the-trpm8-inhibitor-amtb-in-breast-cancer-cells-and-its-identification-as-an-inhibitor-of-voltage-gated-sodium-channels
#10
Kunsala T D S Yapa, Jennifer Deuis, Amelia A Peters, Paraic A Kenny, Sarah J Roberts-Thomson, Irina Vetter, Gregory R Monteith
AIMS: To assess levels of the calcium permeable transient receptor potential cation channel, subfamily melastatin, member 8 (TRPM8) in breast cancer molecular subtypes and to assess the consequences of TRPM8 pharmacological inhibition with AMTB (an inhibitor of TRPM8) on breast cancer cell lines. MATERIALS AND METHODS: Cell viability and migration of breast cancer cells was determined using MTS assays and wound healing assays, respectively. RNA-Seq analysis of breast tumours and qPCR in breast cancer cell lines were used to assess mRNA levels of ion channels...
April 1, 2018: Life Sciences
https://www.readbyqxmd.com/read/29483864/differential-regulation-of-bladder-pain-and-voiding-function-by-sensory-afferent-populations-revealed-by-selective-optogenetic-activation
#11
Jennifer J DeBerry, Vijay K Samineni, Bryan A Copits, Christopher J Sullivan, Sherri K Vogt, Kathryn M Albers, Brian M Davis, Robert W Gereau Iv
Bladder-innervating primary sensory neurons mediate reflex-driven bladder function under normal conditions, and contribute to debilitating bladder pain and/or overactivity in pathological states. The goal of this study was to examine the respective roles of defined subtypes of afferent neurons in bladder sensation and function in vivo via direct optogenetic activation. To accomplish this goal, we generated transgenic lines that express a Channelrhodopsin-2-eYFP fusion protein (ChR2-eYFP) in two distinct populations of sensory neurons: TRPV1-lineage neurons ( Trpv1 Cre ;Ai32, the majority of nociceptors) and Nav 1...
2018: Frontiers in Integrative Neuroscience
https://www.readbyqxmd.com/read/29474819/direct-evidence-for-high-affinity-blockade-of-na-v-1-6-channel-subtype-by-huwentoxin-iv-spider-peptide-using-multiscale-functional-approaches
#12
Tânia C Gonçalves, Rachid Boukaiba, Jordi Molgó, Muriel Amar, Michel Partiseti, Denis Servent, Evelyne Benoit
The Chinese bird spider huwentoxin-IV (HwTx-IV) is well-known to be a highly potent blocker of NaV 1.7 subtype of voltage-gated sodium (NaV ) channels, a genetically validated analgesic target, and thus promising as a potential lead molecule for the development of novel pain therapeutics. In the present study, the interaction between HwTx-IV and NaV 1.6 channel subtype was investigated using multiscale (from in vivo to individual cell) functional approaches. HwTx-IV was approximatively 2 times more efficient than tetrodotoxin (TTX) to inhibit the compound muscle action potential recorded from the mouse skeletal neuromuscular system in vivo, and 30 times more effective to inhibit nerve-evoked than directly-elicited muscle contractile force of isolated mouse hemidiaphragms...
May 1, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29470418/tetrodotoxin-a-candidate-drug-for-nav1-1-induced-mechanical-pain
#13
César Mattei
Tetrodotoxin (TTX), the mode of action of which has been known since the 1960s, is widely used in pharmacology as a specific inhibitor of voltage-gated sodium channels (Nav channels). This toxin has contributed to the characterization of the allosteric model of the Nav channel, and to discriminating TTX-sensitive and TTX-resistant subtypes. In addition to its role as a pharmacological tool, TTX is now considered a therapeutic molecule, and its development should lead to its use in certain pathologies involving Nav channels, particularly in the field of pain...
February 22, 2018: Marine Drugs
https://www.readbyqxmd.com/read/29435993/different-role-of-ttx-sensitive-voltage-gated-sodium-channel-na-v-1-subtypes-in-action-potential-initiation-and-conduction-in-vagal-airway-nociceptors
#14
M Kollarik, H Sun, R A Herbstsomer, F Ru, M Kocmalova, S N Meeker, B J Undem
KEY POINTS: The action potential initiation in the nerve terminals and its subsequent conduction along the axons of afferent nerves are not necessarily dependent on the same voltage-gated sodium channel (NaV 1) subunits. The action potential initiation in jugular C-fibres within airway tissues is not blocked by TTX; nonetheless, conduction of action potentials along the vagal axons of these nerves is often dependent on TTX-sensitive channels. This is not the case for nodose airway Aδ-fibres and C-fibres, where both action potential initiation and conduction is abolished by TTX or selective NaV 1...
April 15, 2018: Journal of Physiology
https://www.readbyqxmd.com/read/29426792/twelve-year-follow-up-of-navigated-computer-assisted-versus-conventional-total-knee-arthroplasty-a-prospective-randomized-comparative-trial
#15
Johannes Cip, Florian Obwegeser, Thomas Benesch, Christian Bach, Paul Ruckenstuhl, Arno Martin
BACKGROUND: Navigated computer-assisted total knee arthroplasty (TKA) was introduced to expedite long-term survival based on improved postoperative implantation accuracy. However, long-term outcome data after 10 years or more are rare, even available meta-analyses show controversial study results. METHODS: In a prospective randomized trial, 100 conventional TKAs (group CONV) were compared with 100 computer-assisted TKAs (group NAV) after a mean follow-up of 12 years postoperatively...
May 2018: Journal of Arthroplasty
https://www.readbyqxmd.com/read/29248843/modulation-of-voltage-gated-sodium-channels-induces-capacitation-in-bull-spermatozoa-through-phosphorylation-of-tyrosine-containing-proteins
#16
Dharmendra Singh Chauhan, Dilip Kumar Swain, Nadeem Shah, Hanuman Prasad Yadav, Abhishek Sharma, Brijesh Yadav, Sarvajeet Yadav, Rajesh Nigam, Satish Kumar Garg
In our previous study, we have reported the molecular presence of Nav 1.8 in bull spermatozoa and its potential involvement in regulation of sperm functions. With the selective blocking of Nav 1.8 using A-803467, alterations in sperm functions were observed, therefore, we envisaged of investigating the involvement of Nav in regulating sperm function and the mechanism(s) involved in it using veratridine, a selective opener of Nav channels. Forty ejaculates were collected from four Hariana bulls and semen samples were pooled in view of the non-significant variations between the different ejaculates...
March 1, 2018: Theriogenology
https://www.readbyqxmd.com/read/29193176/using-voltage-sensor-toxins-and-their-molecular-targets-to-investigate-na-v-1-8-gating
#17
John Gilchrist, Frank Bosmans
Voltage-gated sodium (NaV ) channel gating is a complex phenomenon which involves a distinct contribution of four integral voltage-sensing domains (VSDI, VSDII, VSDIII and VSDIV). Utilizing accrued pharmacological and structural insights, we build on an established chimera approach to introduce animal toxin sensitivity in each VSD of an acceptor channel by transferring in portable S3b-S4 motifs from the four VSDs of a toxin-susceptible donor channel (NaV 1.2). By doing so, we observe that in NaV 1.8, a relatively unexplored channel subtype with distinctly slow gating kinetics, VSDI-III participate in channel opening whereas VSDIV can regulate opening as well as fast inactivation...
November 29, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/29161016/selective-voltage-gated-sodium-channel-peptide-toxins-from-animal-venom-pharmacological-probes-and-analgesic-drug-development
#18
Ying Wu, Hui Ma, Fan Zhang, Chunlei Zhang, Xiaohan Zou, Zhengyu Cao
Voltage-gated sodium channels (Navs) play critical roles in action potential generation and propagation. Nav channelopathy as well as pathological sensitization contribute to allodynia and hyperalgesia. Recent evidence has demonstrated the significant roles of Nav subtypes (Nav1.3, 1.7, 1.8, and 1.9) in nociceptive transduction, and therefore these Navs may represent attractive targets for analgesic drug discovery. Animal toxins are structurally diverse peptides that are highly potent yet selective on ion channel subtypes and therefore represent valuable probes to elucidate the structures, gating properties, and cellular functions of ion channels...
February 21, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29138838/effects-of-scn9a-gene-modification-on-na-channel-and-the-expression-of-nerve-growth-factor-in-a-rat-model-of-diarrhea%C3%A2-predominant-irritable-bowel-syndrome
#19
Yong-Yan Cai, Chen Li, Zhi-Xin Yan, Na Ma, Fang-Fang Li
The aim of the present study was to identify whether the sodium voltage-gated channel alpha subunit 9 (SCN9A) gene modification is a potential treatment for diarrhea‑predominant irritable bowel syndrome (D‑IBS), via regulating the Na+ channel and the expression of nerve growth factor (NGF). The recombinant adenovirus vector of the SCN9A gene was established, and rat colon cells were isolated for SCN9A gene modification. All subjects were divided into four groups: i) The SCN9A‑modified (D‑IBS rat model implanted with SCN9A‑modified colon cells), ii) negative control (NC; D‑IBS rat model implanted with colon cells without SCN9A gene modification), iii) blank (D‑IBS rat model without any treatment) and iv) normal (normal rats without any treatment)...
January 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29134472/real-time-wireless-tumor-tracking-during-breast-conserving-surgery
#20
Natasja Janssen, Roeland Eppenga, Marie-Jeanne Vrancken Peeters, Frederieke van Duijnhoven, Hester Oldenburg, Jos van der Hage, Emiel Rutgers, Jan-Jakob Sonke, Koert Kuhlmann, Theo Ruers, Jasper Nijkamp
PURPOSE: To evaluate a novel surgical navigation system for breast conserving surgery (BCS), based on real-time tumor tracking using the Calypso[Formula: see text] 4D Localization System (Varian Medical Systems Inc., USA). Navigation-guided breast conserving surgery (Nav-BCS) was compared to conventional iodine seed-guided BCS ([Formula: see text]I-BCS). METHODS: Two breast phantom types were produced, containing spherical and complex tumors in which wireless transponders (Nav-BCS) or a iodine seed ([Formula: see text]I-BCS) were implanted...
November 13, 2017: International Journal of Computer Assisted Radiology and Surgery
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