Voltage-Gated Sodium Channel Inhibition by µ-Conotoxins

Toxins (Basel). 2024 Jan 18;16(1):55. doi: 10.3390/toxins16010055.


µ-Conotoxins are small, potent pore-blocker inhibitors of voltage-gated sodium (NaV) channels, which have been identified as pharmacological probes and putative leads for analgesic development. A limiting factor in their therapeutic development has been their promiscuity for different NaV channel subtypes, which can lead to undesirable side-effects. This review will focus on four areas of µ-conotoxin research: (1) mapping the interactions of µ-conotoxins with different NaV channel subtypes, (2) µ-conotoxin structure-activity relationship studies, (3) observed species selectivity of µ-conotoxins and (4) the effects of µ-conotoxin disulfide connectivity on activity. Our aim is to provide a clear overview of the current status of µ-conotoxin research.

Keywords: disulfide-rich peptide; peptide; structure–activity relationships; subtype selectivity; venom peptide; voltage-gated sodium channels; µ-conotoxin.

Publication types

  • Review

MeSH terms

  • Conotoxins* / pharmacology
  • Disulfides
  • Structure-Activity Relationship
  • Voltage-Gated Sodium Channels*


  • Conotoxins
  • Disulfides
  • Voltage-Gated Sodium Channels