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

CA Ahern, J Payandeh, F Bosmans… - Journal of General …, 2016 - rupress.org
Eukaryotic voltage-gated sodium (Nav) channels contribute to the rising phase of action
potentials and served as an early muse for biophysicists laying the foundation for our current …

Role of hERG potassium channel assays in drug development

B Priest, IM Bell, M Garcia - Channels, 2008 - Taylor & Francis
Numerous structurally and functionally unrelated drugs block the hERG potassium channel.
HERG channels are involved in cardiac action potential repolarization, and reduced function …

Ion channels as drug targets: the next GPCRs

GJ Kaczorowski, OB McManus, BT Priest… - The Journal of general …, 2008 - rupress.org
Ion channels are well recognized as important therapeutic targets for treating a number of
different pathophysiologies. Historically, however, development of drugs targeting this …

Characterization of voltage-gated sodium-channel blockers by electrical stimulation and fluorescence detection of membrane potential

CJ Huang, A Harootunian, MP Maher, C Quan… - Nature …, 2006 - nature.com
Voltage-gated ion channels regulate many physiological functions and are targets for a
number of drugs. Patch-clamp electrophysiology is the standard method for measuring …

Deep Mutational Scan of an SCN5A Voltage Sensor

AM Glazer, BM Kroncke, KA Matreyek… - Circulation: Genomic …, 2020 - Am Heart Assoc
Background: Variants in ion channel genes have classically been studied in low throughput
by patch clamping. Deep mutational scanning is a complementary approach that can …

High-throughput electrophysiological assays for voltage gated ion channels using SyncroPatch 768PE

T Li, G Lu, EY Chiang, T Chernov-Rogan, JL Grogan… - PLoS …, 2017 - journals.plos.org
Ion channels regulate a variety of physiological processes and represent an important class
of drug target. Among the many methods of studying ion channel function, patch clamp …

Discovery of a novel class of benzazepinone Nav1. 7 blockers: potential treatments for neuropathic pain

SB Hoyt, C London, D Gorin, MJ Wyvratt… - Bioorganic & medicinal …, 2007 - Elsevier
A series of benzodiazepines and benzazepinones were synthesized and evaluated as
potential sodium channel blockers in a functional, membrane potential-based assay. One …

Animal toxins influence voltage-gated sodium channel function

J Gilchrist, BM Olivera, F Bosmans - Voltage Gated Sodium Channels, 2014 - Springer
Voltage-gated sodium (Nav) channels are essential contributors to neuronal excitability,
making them the most commonly targeted ion channel family by toxins found in animal …

[HTML][HTML] Sodium channel blockers for the treatment of neuropathic pain

A Bhattacharya, AD Wickenden, SR Chaplan - Neurotherapeutics, 2009 - Elsevier
Drugs that block voltage-gated sodium channels are efficacious in the management of
neuropathic pain. Accordingly, this class of ion channels has been a major focus of …

An introduction to pain pathways and pain “targets”

V Das - Progress in molecular biology and translational …, 2015 - Elsevier
The purpose of this chapter is to provide a brief introduction to the anatomy and physiology
of pain pathways from peripheral nociceptors to central nervous system areas involved in …