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Papers of the Week


Papers: 27 Jan 2024 - 2 Feb 2024


2024 Jan 25


Curr Opin Pharmacol


38277942


75

Analgesic potential of voltage gated sodium channel modulators for the management of pain.

Authors

McDougall JJ, O'Brien MS

Abstract

Neuronal electrochemical signals involve the flux of sodium ions through voltage-gated sodium channels (Na) located in the neurolemma. Of the nine sodium channel subtypes, Na-1.7, 1.8, and 1.9 are predominantly located on nociceptors, making them prime targets to control pain. This review highlights some of the latest discoveries targeting Na channel activity, including: (1) charged local anaesthetic derivatives; (2) Na channel toxins and associated small peptide blockers; (3) regulation of Na channel accessory proteins; and (4) genetic manipulation of Na channel function. While the translation of preclinical findings to a viable treatment in humans has remained a challenge, a greater understanding of Na channel physiology could lead to the development of a new stream of therapies aimed at alleviating chronic pain.