Status of peripheral sodium channel blockers for non-addictive pain treatment

M Alsaloum, GP Higerd, PR Effraim… - Nature Reviews …, 2020 - nature.com
The effective and safe treatment of pain is an unmet health-care need. Current medications
used for pain management are often only partially effective, carry dose-limiting adverse …

iPSCs and DRGs: stepping stones to new pain therapies

M Alsaloum, SG Waxman - Trends in molecular medicine, 2022 - cell.com
There is a pressing need for more effective nonaddictive treatment options for pain. Pain
signals are transmitted from the periphery into the spinal cord via dorsal root ganglion (DRG) …

Understanding the physiological role of NaV1. 9: Challenges and opportunities for pain modulation

W Brackx, R de Cássia Collaço, M Theys… - Pharmacology & …, 2023 - Elsevier
Abstract Voltage-activated Na+(Na V) channels are crucial contributors to rapid electrical
signaling in the human body. As such, they are among the most targeted membrane proteins …

Reduced pain sensitivity of episodic pain syndrome model mice carrying a Nav1. 9 mutation by ANP-230, a novel sodium channel blocker

H Okuda, S Inoue, Y Oyamada, A Koizumi… - Heliyon, 2023 - cell.com
The sodium channel Nav1. 9 is expressed in the sensory neurons of small diameter dorsal
root ganglia that transmit pain signals, and gain-of-function Nav1. 9 mutations have been …

Direct fluorescent labeling of NF186 and NaV1. 6 in living primary neurons using bioorthogonal click chemistry

N Stajković, Y Liu, A Arsić, N Meng… - Journal of Cell …, 2023 - journals.biologists.com
The axon initial segment (AIS) is a highly specialized neuronal compartment that regulates
the generation of action potentials and maintenance of neuronal polarity. Live imaging of the …

[HTML][HTML] ErbB1-dependent signalling and vesicular trafficking in primary afferent nociceptors associated with hypersensitivity in neuropathic pain

R Mitchell, M Mikolajczak, C Kersten… - Neurobiology of …, 2020 - Elsevier
Effective analgesic treatment for neuropathic pain remains an unmet need, so previous
evidence that epidermal growth factor receptor inhibitors (EGFRIs) provide unexpected rapid …

[HTML][HTML] Unique electrophysiological property of a novel Nav1. 7, Nav1. 8, and Nav1. 9 sodium channel blocker, ANP-230

T Kamei, T Kudo, H Yamane, F Ishibashi… - Biochemical and …, 2024 - Elsevier
Voltage-gated sodium channel subtypes, Nav1. 7, Nav1. 8, and Nav1. 9 are predominantly
expressed in peripheral sensory neurons. Recent genetic studies have revealed that they …

Characterization of Synthetic Tf2 as a NaV1.3 Selective Pharmacological Probe

MR Israel, TS Dash, SN Bothe, SD Robinson, JR Deuis… - Biomedicines, 2020 - mdpi.com
NaV1. 3 is a subtype of the voltage-gated sodium channel family. It has been implicated in
the pathogenesis of neuropathic pain, although the contribution of this channel to neuronal …

Pharmacological activity and NMR solution structure of the leech peptide HSTX-I

KL McMahon, B Tay, JR Deuis, BS Tanaka… - Biochemical …, 2020 - Elsevier
The role of voltage-gated sodium (Na V) channels in pain perception is indisputable. Of
particular interest as targets for the development of pain therapeutics are the tetrodotoxin …

Homozygous C-terminal loss-of-function NaV1. 4 variant in a patient with congenital myasthenic syndrome

A Echaniz-Laguna, V Biancalana… - Journal of Neurology …, 2020 - jnnp.bmj.com
Results We report a 25-year-old consanguineous Turkish woman who presented from
infancy with fluctuating stridor, dysphonia, dyspnoea and limb weakness that persisted for …