Development of a Rapid Throughput Assay for Identification of hNav1.7 Antagonist Using Unique Efficacious Sodium Channel Agonist, Antillatoxin

scientific article published on 16 February 2016

Development of a Rapid Throughput Assay for Identification of hNav1.7 Antagonist Using Unique Efficacious Sodium Channel Agonist, Antillatoxin is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.3390/MD14020036
P932PMC publication ID4771989
P698PubMed publication ID26891306
P5875ResearchGate publication ID295078479

P50authorXichun LiQ86926084
P2093author name stringMasayuki Inoue
Fan Zhang
Zhengyu Cao
Fang Zhao
Liang Jin
Boyang Yu
P2860cites workAntillatoxin is a sodium channel activator that displays unique efficacy in heterologously expressed rNav1.2, rNav1.4 and rNav1.5 α subunitsQ21262973
Nociceptor-specific gene deletion reveals a major role for Nav1.7 (PN1) in acute and inflammatory painQ24562888
Distinct Nav1.7-dependent pain sensations require different sets of sensory and sympathetic neuronsQ24632552
Mutations in SCN9A, encoding a sodium channel alpha subunit, in patients with primary erythermalgiaQ24675844
Developmental neurotoxicity of pyrethroid insecticides: critical review and future research needsQ24814126
The riluzole derivative 2-amino-6-trifluoromethylthio-benzothiazole (SKA-19), a mixed KCa2 activator and NaV blocker, is a potent novel anticonvulsantQ27339255
Nomenclature of voltage-gated sodium channelsQ28141860
Alternative statistical parameter for high-throughput screening assay quality assessmentQ28283010
Common molecular determinants of local anesthetic, antiarrhythmic, and anticonvulsant block of voltage-gated Na+ channelsQ28379121
Phenytoin inhibits the persistent sodium current in neocortical neurons by modifying its inactivation propertiesQ28485346
Identification of PN1, a predominant voltage-dependent sodium channel expressed principally in peripheral neuronsQ28569751
Endogenous expression of the beta1A sodium channel subunit in HEK-293 cellsQ40879597
Basis of the antiseizure action of phenytoinQ41289597
Lidocaine block of cardiac sodium channelsQ41556598
Diphenytoin, riluzole and lidocaine: three sodium channel blockers, with different mechanisms of action, decrease hippocampal epileptiform activityQ42273460
Slow closed-state inactivation: a novel mechanism underlying ramp currents in cells expressing the hNE/PN1 sodium channel.Q42686664
Increase of sodium current after pyrethroid insecticides in mouse neuroblastoma cellsQ44204489
In silico docking reveals possible Riluzole binding sites on Nav1.6 sodium channel: implications for amyotrophic lateral sclerosis therapyQ45735872
Carbamazepine inhibition of neuronal Na+ currents: quantitative distinction from phenytoin and possible therapeutic implicationsQ48697139
Validation of FLIPR membrane potential dye for high throughput screening of potassium channel modulators.Q53677715
Slow binding of phenytoin to inactivated sodium channels in rat hippocampal neurons.Q54022626
Effects of veratridine on sodium currents and fluxes.Q54137279
A critical role for transmembrane segment IVS6 of the sodium channel alpha subunit in fast inactivationQ72223457
A common anticonvulsant binding site for phenytoin, carbamazepine, and lamotrigine in neuronal Na+ channelsQ77388391
A pharmacophore derived phenytoin analogue with increased affinity for slow inactivated sodium channels exhibits a desired anticonvulsant profileQ30441260
High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1.Q30478958
Sodium channel inhibitor drug discovery using automated high throughput electrophysiology platformsQ33400498
Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2Q33417208
Human embryonic kidney (HEK293) cells express endogenous voltage-gated sodium currents and Na v 1.7 sodium channelsQ33625778
Antillatoxin and kalkitoxin, ichthyotoxins from the tropical cyanobacterium Lyngbya majuscula, induce distinct temporal patterns of NMDA receptor-mediated neurotoxicityQ33873690
A novel Nav1.7 mutation producing carbamazepine-responsive erythromelalgiaQ33918510
Voltage-gated sodium channels as therapeutic targetsQ33925684
Antillatoxin is a marine cyanobacterial toxin that potently activates voltage-gated sodium channelsQ33952224
Voltage-gated ion channels and gating modifier toxins.Q34161355
Identification of human Ether-à-go-go related gene modulators by three screening platforms in an academic drug-discovery setting.Q34407398
Gain-of-function mutation in Nav1.7 in familial erythromelalgia induces bursting of sensory neuronsQ34426737
Differential action of riluzole on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels.Q34435972
Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channelQ34461603
On the use of neuro-2a neuroblastoma cells versus intact neurons in primary culture for neurotoxicity studiesQ34470161
Overview of molecular relationships in the voltage-gated ion channel superfamily.Q34480285
Mechanisms of use-dependent block of sodium channels in excitable membranes by local anestheticsQ34534868
High-throughput fluorescent-based NKCC functional assay in adherent epithelial cells.Q34626292
Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reactionQ34684384
The investigational anticonvulsant lacosamide selectively enhances slow inactivation of voltage-gated sodium channels.Q34701722
High-throughput electrophysiology: an emerging paradigm for ion-channel screening and physiologyQ34763903
Integration of virtual and high-throughput screeningQ34988235
The twisted side chain of antillatoxin is important for potent toxicity: total synthesis and biological evaluation of antillatoxin and analoguesQ35016849
Differential modulation of Nav1.7 and Nav1.8 peripheral nerve sodium channels by the local anesthetic lidocaineQ35047167
Additivity of pyrethroid actions on sodium influx in cerebrocortical neurons in primary cultureQ35591794
Intra- and interfamily phenotypic diversity in pain syndromes associated with a gain-of-function variant of NaV1.7.Q35642815
Properties of human brain sodium channel α-subunits expressed in HEK293 cells and their modulation by carbamazepine, phenytoin and lamotrigineQ37585424
Lidocaine reduces the transition to slow inactivation in Na(v)1.7 voltage-gated sodium channelsQ38649763
Influence of lipid-soluble gating modifier toxins on sodium influx in neocortical neuronsQ39964248
A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptorsQ40028879
Cellular HTS assays for pharmacological characterization of Na(V)1.7 modulatorsQ40035901
Automated ion channel screening: patch clamping made easyQ40156501
The natural scorpion peptide, BmK NT1 activates voltage-gated sodium channels and produces neurotoxicity in primary cultured cerebellar granule cells.Q40283974
Carbamazepine interacts with a slow inactivation state of NaV1.8-like sodium channelsQ40288025
Functional assay of voltage-gated sodium channels using membrane potential-sensitive dyes.Q40529990
Overexpression of T-type calcium channels in HEK-293 cells increases intracellular calcium without affecting cellular proliferationQ40865162
P275copyright licenseCreative Commons Attribution 4.0 InternationalQ20007257
P6216copyright statuscopyrightedQ50423863
P433issue2
P577publication date2016-02-16
P1433published inMarine DrugsQ2122804
P1476titleDevelopment of a Rapid Throughput Assay for Identification of hNav1.7 Antagonist Using Unique Efficacious Sodium Channel Agonist, Antillatoxin
P478volume14

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cites work (P2860)
Q39126913Bringing new dimensions to drug discovery screening: impact of cellular stimulation technologies
Q90019912Dehydrocrenatidine Inhibits Voltage-Gated Sodium Channels and Ameliorates Mechanic Allodia in a Rat Model of Neuropathic Pain
Q41045838Effects of Tetrodotoxin in Mouse Models of Visceral Pain.
Q90451672Emerging neurotechnology for antinoceptive mechanisms and therapeutics discovery
Q49306666Mechanism-specific assay design facilitates the discovery of Nav1.7-selective inhibitors.
Q48353819Phenytoin: a step by step insight into its multiple mechanisms of action-80 years of mechanistic studies in neuropharmacology.
Q48337085Sodium channels and pain: from toxins to therapies
Q89296981Veratridine modifies the gating of human voltage-gated sodium channel Nav1.7.

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