Neuropathic pain: preclinical and early clinical progress with voltage-gated sodium channel blockers

Structures of human Nav1.7 channel in complex with auxiliary subunits and animal toxins

(2019) Huaizong Shen et al.   SCIENCE

Revisiting Tramadol: A Multi-Modal Agent for Pain Management

(2019) Ahmed Barakat   CNS DRUGS

Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study in Healthy Volunteers

(2019) Michael E. Rothenberg et al.   CLINICAL DRUG INVESTIGATION

1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of Na V 1.7 inhibition

(2018) Alessandro A. Boezio et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Assessment of efficacy and safety of eslicarbazepine acetate for the treatment of trigeminal neuralgia

(2018) A. Sanchez-Larsen et al.   EUROPEAN JOURNAL OF PAIN

HNTX-III Alleviates Inflammatory and Neuropathic Pain in Animal Models

(2018) Yu Liu et al.   International Journal of Peptide Research and Therapeutics

Old Friends With New Faces: Are Sodium Channel Blockers the Future of Adjunct Pain Medication Management?

(2018) Ashley M. Thomas et al.   JOURNAL OF PAIN

Effect of Tetrodotoxin Pellets in a Rat Model of Postherpetic Neuralgia

(2018) Bihong Hong et al.   Marine Drugs

Efficacy of the Nav1.7 blocker PF-05089771 in a randomised, placebo-controlled, double-blind clinical study in subjects with painful diabetic peripheral neuropathy

(2018) Aoibhinn McDonnell et al.   PAIN

Inhibition of the Ubc9 E2 SUMO-conjugating enzyme–CRMP2 interaction decreases NaV1.7 currents and reverses experimental neuropathic pain

(2018) Liberty François-Moutal et al.   PAIN

Opiate-Free Pain Therapy Using Carbamazepine-Loaded Microparticles Provides Up to 2 Weeks of Pain Relief in a Neuropathic Pain Model

(2018) Haining Dai et al.   Pain Practice

GpTx-1 and [Ala5 , Phe6 , Leu26 , Arg28 ]GpTx-1, two peptide NaV 1.7 inhibitors: analgesic and tolerance properties at the spinal level

(2018) Chao Chen et al.   BRITISH JOURNAL OF PHARMACOLOGY

Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain

(2018) Girish Bankar et al.   Cell Reports

µ-TRTX-Ca1a: a novel neurotoxin from Cyriopagopus albostriatus with analgesic effects

(2018) Yun-xiao Zhang et al.   ACTA PHARMACOLOGICA SINICA

Lacosamide in patients with Nav1.7 mutations-related small fibre neuropathy: a randomized controlled trial

(2018) Bianca T A de Greef et al.   BRAIN

Pain relief in a neuropathy patient by lacosamide: Proof of principle of clinical translation from patient-specific iPS cell-derived nociceptors

(2018) Barbara Namer et al.   EBioMedicine

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

(2017) Russell F. Graceffa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Safety and efficacy of a Nav1.7 selective sodium channel blocker in patients with trigeminal neuralgia: a double-blind, placebo-controlled, randomised withdrawal phase 2a trial

(2017) Joanna M Zakrzewska et al.   LANCET NEUROLOGY

µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential

(2017) Elisabetta Tosti et al.   Marine Drugs

Emerging therapies for neuropathic pain

(2017) Didier Bouhassira et al.   PAIN

Sodium channels in pain disorders

(2017) Sulayman D. Dib-Hajj et al.   PAIN

Na V 1.7 as a pain target – From gene to pharmacology

(2017) Irina Vetter et al.   PHARMACOLOGY & THERAPEUTICS

Tetrodotoxin for Moderate to Severe Cancer-Related Pain: A Multicentre, Randomized, Double-Blind, Placebo-Controlled, Parallel-Design Trial

(2017) Neil A. Hagen et al.   Pain Research & Management

Topical phenytoin for the treatment of neuropathic pain

(2017) David Kopsky et al.   Journal of Pain Research

Neuropathic pain

(2017) Luana Colloca et al.   Nature Reviews Disease Primers

Recent Trends in the Discovery of Small Molecule Blockers of Sodium Channels

(2016) Roberta Gualdani et al.   CURRENT MEDICINAL CHEMISTRY

Nav1.7 and other voltage-gated sodium channels as drug targets for pain relief

(2016) Edward C Emery et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

A Gain-of-Function Mutation in Nav1.6 in a Case of Trigeminal Neuralgia

(2016) Brian S Tanaka et al.   MOLECULAR MEDICINE

A SCN10A SNP biases human pain sensitivity

(2016) Guangyou Duan et al.   Molecular Pain

Translational neuropathic pain research: A clinical perspective

(2016) D. Bouhassira et al.   NEUROSCIENCE

Neuropathic pain

(2016) Nanna B. Finnerup et al.   PAIN

Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia

(2016) Lishuang Cao et al.   Science Translational Medicine

Voltage-Gated Ion Channels in the PNS: Novel Therapies for Neuropathic Pain?

(2016) Gareth R. Tibbs et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain

(2016) Jennifer Deuis et al.   Toxins

Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release

(2016) Aristos J. Alexandrou et al.   PLoS One

A novel selective and orally bioavailable Nav1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability

(2015) Claire Elizabeth Payne et al.   BRITISH JOURNAL OF PHARMACOLOGY

Voltage gated sodium channels as drug discovery targets

(2015) Sharan K Bagal et al.   Channels

Rufinamide Improves Functional and Behavioral Deficits via Blockade of Tetrodotoxin-Resistant Sodium Channels in Diabetic Neuropathy

(2015) Shivsharan Kharatmal et al.   CURRENT NEUROVASCULAR RESEARCH

Voltage-gated sodium channels

(2015) Kevin Kwong et al.   CURRENT OPINION IN PHARMACOLOGY

Novel sodium channel antagonists in the treatment of neuropathic pain

(2015) Mirko Rivara et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

The hitchhiker’s guide to the voltage-gated sodium channel galaxy

(2015) Christopher A. Ahern et al.   JOURNAL OF GENERAL PHYSIOLOGY

Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications

(2015) Manuel de Lera Ruiz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Engineering Potent and Selective Analogues of GpTx-1, a Tarantula Venom Peptide Antagonist of the NaV1.7 Sodium Channel

(2015) Justin K. Murray et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacotherapy for neuropathic pain in adults: a systematic review and meta-analysis

(2015) Nanna B Finnerup et al.   LANCET NEUROLOGY

NaV1.9: a sodium channel linked to human pain

(2015) Sulayman D. Dib-Hajj et al.   NATURE REVIEWS NEUROSCIENCE

Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist

(2015) S. Ahuja et al.   SCIENCE

Endogenous opioids contribute to insensitivity to pain in humans and mice lacking sodium channel Nav1.7

(2015) Michael S. Minett et al.   Nature Communications

A Monoclonal Antibody that Targets a NaV1.7 Channel Voltage Sensor for Pain and Itch Relief

(2014) Jun-Ho Lee et al.   CELL

Painful neuropathies: the emerging role of sodium channelopathies

(2014) Brigitte A. Brouwer et al.   JOURNAL OF THE PERIPHERAL NERVOUS SYSTEM

The effect of oxcarbazepine in peripheral neuropathic pain depends on pain phenotype: A randomised, double-blind, placebo-controlled phenotype-stratified study

(2014) Dyveke T. Demant et al.   PAIN

Synthesis and Analgesic Effects of μ-TRTX-Hhn1b on Models of Inflammatory and Neuropathic Pain

(2014) Yu Liu et al.   Toxins

Neuropathic pain in the general population: A systematic review of epidemiological studies

(2013) O. van Hecke et al.   PAIN

Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels

(2013) K. McCormack et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery of a selective NaV1.7 inhibitor from centipede venom with analgesic efficacy exceeding morphine in rodent pain models

(2013) S. Yang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Advances in Targeting Voltage-Gated Sodium Channels with Small Molecules

(2012) Antonio Nardi et al.   ChemMedChem

Methylglyoxal modification of Nav1.8 facilitates nociceptive neuron firing and causes hyperalgesia in diabetic neuropathy

(2012) Angelika Bierhaus et al.   NATURE MEDICINE

The NaV1.7 sodium channel: from molecule to man

(2012) Sulayman D. Dib-Hajj et al.   NATURE REVIEWS NEUROSCIENCE

Nav1.8 expression is not restricted to nociceptors in mouse peripheral nervous system

(2012) Shannon D. Shields et al.   PAIN

Gain of function NaV1.7 mutations in idiopathic small fiber neuropathy

(2011) Catharina G. Faber et al.   ANNALS OF NEUROLOGY

Treatment of Nav1.7-mediated pain in inherited erythromelalgia using a novel sodium channel blocker

(2011) Yigal Paul Goldberg et al.   PAIN

Adjuvant analgesics in neuropathic pain

(2009) Vincent KF Kong et al.   EUROPEAN JOURNAL OF ANAESTHESIOLOGY

Voltage-Gated Sodium Channels: Therapeutic Targets for Pain

(2009) Sulayman D. Dib-Hajj et al.   PAIN MEDICINE

Tetrodotoxin-resistant voltage-gated sodium channels Nav1.8 and Nav1.9 are expressed in the retina

(2008) Brendan J. O'Brien et al.   JOURNAL OF COMPARATIVE NEUROLOGY

Practice Parameter: The diagnostic evaluation and treatment of trigeminal neuralgia (an evidence-based review): Report of the Quality Standards Subcommittee of the American Academy of Neurology and the European Federation of Neurological Societies

(2008) G. Gronseth et al.   NEUROLOGY