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

Curr Opin Pharmacol. 2024 Jan 25;75:102433. doi: 10.1016/j.coph.2024.102433. Online ahead of print.ABSTRACTNeuronal electrochemical signals involve the flux of sodium ions through voltage-gated sodium channels (NaV) located in the neurolemma. Of the nine sodium channel subtypes, NaV-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 NaV channel activity, including: (1) charged local anaesthetic derivatives; (2) NaV channel toxins and associated small peptide blockers; (3) regulation of NaV channel accessory proteins; and (4) genetic manipulation of NaV channel function. While the translation of preclinical findings to a viable treatment in humans has remained a challenge, a greater understanding of NaV channel physiology could lead to the development of a new stream of therapies aimed at alleviating chronic pain.PMID:38277942 | DOI:10.1016/j.coph.2024.102433
Source: Current Opinion in Pharmacology - Category: Drugs & Pharmacology Authors: Source Type: research