Lidocaine Binding Enhances Inhibition of Nav1.7 Channels by the Sulfonamide PF-05089771

Structural basis for antiarrhythmic drug interactions with the human cardiac sodium channel

(2019) Phuong T. Nguyen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery of morpholine-based aryl sulfonamides as Na v 1.7 inhibitors

(2018) Yong-Jin Wu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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 hNaV1.7 Inhibitors for the Treatment of Pain

(2018) Thilo Focken et al.   JOURNAL OF MEDICINAL CHEMISTRY

Mechanism-specific assay design facilitates the discovery of Nav1.7-selective inhibitors

(2018) Tania Chernov-Rogan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of Selective Acyl Sulfonamide–Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (NaV) 1.7 with Potent Analgesic Activity

(2018) Shaoyi Sun et al.   JOURNAL OF MEDICINAL CHEMISTRY

Regulation of Na+channel inactivation by the DIII and DIV voltage-sensing domains

(2017) Eric J. Hsu et al.   JOURNAL OF GENERAL PHYSIOLOGY

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

Lacosamide Inhibition of Nav1.7 Voltage-Gated Sodium Channels: Slow Binding to Fast-Inactivated States

(2017) Sooyeon Jo et al.   MOLECULAR PHARMACOLOGY

Insensitivity to pain induced by a potent selective closed-state Nav1.7 inhibitor

(2017) M. Flinspach et al.   Scientific Reports

Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models

(2016) Thilo Focken et al.   ACS Medicinal Chemistry Letters

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

Neosaxitoxin in Rat Sciatic Block

(2015) Jay S. Templin et al.   ANESTHESIOLOGY

A Phase 1, Dose-escalation, Double-blind, Block-randomized, Controlled Trial of Safety and Efficacy of Neosaxitoxin Alone and in Combination with 0.2% Bupivacaine, with and without Epinephrine, for Cutaneous Anesthesia

(2015) Kimberly Lobo et al.   ANESTHESIOLOGY

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

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

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

(2015) S. Ahuja et al.   SCIENCE

Recent progress in sodium channel modulators for pain

(2014) Sharan K. Bagal et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Domain IV voltage-sensor movement is both sufficient and rate limiting for fast inactivation in sodium channels

(2013) Deborah L. Capes et al.   JOURNAL OF GENERAL PHYSIOLOGY

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

Modulation of neuronal sodium channels by the sea anemone peptide BDS-I

(2012) Pin Liu et al.   JOURNAL OF NEUROPHYSIOLOGY

Gating transitions in the selectivity filter region of a sodium channel are coupled to the domain IV voltage sensor

(2012) D. L. Capes et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Lidocaine reduces the transition to slow inactivation in Nav1.7 voltage-gated sodium channels

(2011) Patrick L Sheets et al.   BRITISH JOURNAL OF PHARMACOLOGY

Inhibition of Neuronal Voltage-Gated Sodium Channels by Brilliant Blue G

(2011) S. Jo et al.   MOLECULAR PHARMACOLOGY

The Sodium Channel as a Target for Local Anesthetic Drugs

(2011) Harry A. Fozzard et al.   Frontiers in Pharmacology

Fast- or Slow-inactivated State Preference of Na+ Channel Inhibitors: A Simulation and Experimental Study

(2010) Robert Karoly et al.   PLoS Computational Biology

Local Anesthetics Disrupt Energetic Coupling between the Voltage-sensing Segments of a Sodium Channel

(2008) Yukiko Muroi et al.   JOURNAL OF GENERAL PHYSIOLOGY