PMID

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Article Title

Organization

Inhibition of veratridine-induced delayed inactivation of the voltage-sensitive sodium channel by synthetic analogs of crambescin B.

Tohoku University

[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.

TBA

Sulfonamides as Selective Na

Amgen

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

Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.

University Of Oxford

Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.

Novartis Institutes For Biomedical Research

Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.

University College London

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.

Astrazeneca

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Abbott Laboratories

Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.

The Scripps Research Institute

Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.

Cambridge Neuroscience

 

Batrachotoxin binding site antagonists

TBA

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 of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.

Abbott Laboratories

Sodium channel blockers.

Purdue Pharma

Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers.

Cenes Pharmaceuticals

Anticonvulsant activity of piperidinol and (dialkylamino)alkanol esters.

TBA

Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.

Yogi Vemana University

Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.

University Of Leipzig

Inhibitors of HIV-1 proteinase containing 2-heterosubstituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, enzyme inhibition, and antiviral activity.

Sandoz Forschungsinstitut Ges.M.B.H.