Nav1.7 target modulation and efficacy can be measured in nonhuman primate assays

Fifteen years of Na V 1.7 channels as an analgesic target: Why has excellent in vitro pharmacology not translated into in vivo analgesic efficacy?

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Defining the Functional Role of NaV1.7 in Human Nociception

(2019) Lucy A. McDermott et al.   NEURON

Moving to a World Beyond “p 

(2019) Ronald L. Wasserstein et al.   AMERICAN STATISTICIAN

The Role of Voltage-Gated Sodium Channels in Pain Signaling

(2019) David L. Bennett et al.   PHYSIOLOGICAL REVIEWS

Lack of Detection of the Analgesic Properties of PF‐05089771, a Selective Na v 1.7 Inhibitor, Using a Battery of Pain Models in Healthy Subjects

(2019) Pieter Siebenga et al.   CTS-Clinical and Translational Science

Microneurography - how it started and how it works

(2018) Åke Bernhard Vallbo   JOURNAL OF NEUROPHYSIOLOGY

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

fMRI study of the role of glutamate NMDA receptor in the olfactory processing in monkeys

(2018) Fuqiang Zhao et al.   PLoS One

Na V 1.7 as a Pharmacogenomic Target for Pain: Moving Toward Precision Medicine

(2018) Yang Yang et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Pharmacological validation of a novel nonhuman primate measure of thermal responsivity with utility for predicting analgesic effects

(2018) Joshua D Vardigan et al.   Journal of Pain Research

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 NaV1.7

(2017) Nigel. A. Swain et al.   JOURNAL OF MEDICINAL CHEMISTRY

Breaking barriers to novel analgesic drug development

(2017) Ajay S. Yekkirala et al.   NATURE REVIEWS DRUG DISCOVERY

High-Throughput Screening of NaV1.7 Modulators Using a Giga-Seal Automated Patch Clamp Instrument

(2016) Chris Chambers et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Clinical Micro-Dose Studies to Explore the Human Pharmacokinetics of Four Selective Inhibitors of Human Nav1.7 Voltage-Dependent Sodium Channels

(2016) Hannah M. Jones et al.   CLINICAL PHARMACOKINETICS

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

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

Pharmacological Management of Chronic Neuropathic Pain: Revised Consensus Statement from the Canadian Pain Society

(2016) DE Moulin et al.   Pain Research & Management

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

Functional imaging of olfaction by CBV fMRI in monkeys: Insight into the role of olfactory bulb in habituation

(2015) Fuqiang Zhao et al.   NEUROIMAGE

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

(2015) S. Ahuja et al.   SCIENCE

Painful and painless channelopathies

(2014) David L H Bennett et al.   LANCET NEUROLOGY

Regulating excitability of peripheral afferents: emerging ion channel targets

(2014) Stephen G Waxman et al.   NATURE NEUROSCIENCE

Global Nav1.7 Knockout Mice Recapitulate the Phenotype of Human Congenital Indifference to Pain

(2014) Jacinthe Gingras et al.   PLoS One

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

Expression of Nav1.7 in DRG Neurons Extends from Peripheral Terminals in the Skin to Central Preterminal Branches and Terminals in the Dorsal Horn

(2012) Joel A Black et al.   Molecular Pain

Evaluation of Anticonvulsants for Possible Use in Neuropathic Pain

(2011) A. M. Waszkielewicz et al.   CURRENT MEDICINAL CHEMISTRY

Nav1.7 is the Predominant Sodium Channel in Rodent Olfactory Sensory Neurons

(2011) Hye-Sook Ahn et al.   Molecular Pain

Channelopathies have many faces

(2011) Stephen G. Waxman   NATURE

Loss-of-function mutations in sodium channel Nav1.7 cause anosmia

(2011) Jan Weiss et al.   NATURE

Block of Neuronal Na+ Channels by Antidepressant Duloxetine in a State-dependent Manner

(2010) Sho-Ya Wang et al.   ANESTHESIOLOGY

Sodium Channels in Normal and Pathological Pain

(2010) Sulayman D. Dib-Hajj et al.   Annual Review of Neuroscience

Nociceptors: the sensors of the pain pathway

(2010) Adrienne E. Dubin et al.   JOURNAL OF CLINICAL INVESTIGATION

Cellular and Molecular Mechanisms of Pain

(2009) Allan I. Basbaum et al.   CELL

Microneurography in rats: A minimally invasive method to record single C-fiber action potentials from peripheral nerves in vivo

(2009) Jordi Serra et al.   NEUROSCIENCE LETTERS

Differential Block of Sensory Neuronal Voltage-Gated Sodium Channels by Lacosamide [(2R)-2-(Acetylamino)-N-benzyl-3-methoxypropanamide], Lidocaine, and Carbamazepine

(2008) P. L. Sheets et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS