70 articles for thisTarget
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Inhibition of veratridine-induced delayed inactivation of the voltage-sensitive sodium channel by synthetic analogs of crambescin B.
Tohoku University
Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.
Gilead Sciences
Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.
Xenon Pharmaceuticals
Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation.
Merck Research Laboratories
Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications.
Merck Research Laboratories
Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.
Merck Research Laboratories
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.
Pfizer
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Novartis Institutes For Biomedical Research
Studies examining the relationship between the chemical structure of protoxin II and its activity on voltage gated sodium channels.
Purdue Pharma
Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.
University College London
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
Astrazeneca
Novel, broad-spectrum anticonvulsants containing a sulfamide group: advancement of N-((benzo[b]thien-3-yl)methyl)sulfamide (JNJ-26990990) into human clinical studies.
Johnson & Johnson Pharmaceutical Research & Development
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Cambridge Neuroscience
Design, synthesis, and pharmacological evaluation of conformationally constrained analogues of N,N'-diaryl- and N-aryl-N-aralkylguanidines as potent inhibitors of neuronal Na+ channels.
Cambridge Neuroscience
Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers.
Warner-Lambert
Lactam-stabilized helical analogues of the analgesicµ-conotoxin KIIIA.
Monash University
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.
Abbott Laboratories
Anticonvulsant activity of 2,4(1H)-diarylimidazoles in mice and rats acute seizure models.
Università
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Abbott Laboratories
Synthesis and characterization of N-(acenaphth-5-yl)-N'-(4-methoxynaphth-1-yl)guanidine as a glutamate release inhibitor and potential anti-ischemic agent
TBA
2,4(5)-diarylimidazoles as inhibitors of hNaV1.2 sodium channels: pharmacological evaluation and structure-property relationships.
Università
Discovery and stereoselective synthesis of the novel isochroman neurokinin-1 receptor antagonist 'CJ-17,493'.
Pfizer
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.
Abbott Laboratories
Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels.
University of Utah
Advances in Epilepsy: Mechanisms, Clinical Trials, and Drug Therapies.
Sichuan University
Optimization of the Antibacterial Spectrum and the Developability Profile of the Novel-Class Natural Product Corramycin.
Evotec
Identification of Selective Acyl Sulfonamide-Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (Na
Xenon Pharmaceuticals
Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Na
Abbvie
Functional Characterization of the Nemertide α Family of Peptide Toxins.
Uppsala University
Identification of aryl sulfonamides as novel and potent inhibitors of Na
Xenon Pharmaceuticals
Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I
Gilead Sciences
Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers.
Cenes Pharmaceuticals
Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.
Amgen
Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na
Bristol-Myers Squibb Research and Development
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
Siteone Therapeutics
A structure-activity relationship study of novel phenylacetamides which are sodium channel blockers.
Warner-Lambert
Synthesis and evaluation of a 125I-labeled iminodihydroquinoline-derived tracer for imaging of voltage-gated sodium channels.
Institute of Nuclear Medicine
Expanding chemical diversity of conotoxins: peptoid-peptide chimeras of the sodium channel blocker μ-KIIIA and its selenopeptide analogues.
University of Gdansk
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa
Xenon Pharmaceuticals
Discovery of morpholine-based aryl sulfonamides as Na
Bristol-Myers Squibb Research and Development
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.
Idorsia Pharmaceuticals
Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na
Icagen
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors
Ctxt
In vitro and in vivo pharmacological characterization of BM-613 [N-n-pentyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl]urea], a novel dual thromboxane synthase inhibitor and thromboxane receptor antagonist.
University of Li&Eagrove;Ge
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Duquesne University
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
Kochi Medical School