Arthropod toxins and their antinociceptive properties: From venoms to painkillers

Pharmacol Ther. 2018 Aug:188:176-185. doi: 10.1016/j.pharmthera.2018.03.007. Epub 2018 Mar 29.

Abstract

The complex process of pain control commonly involves the use of systemic analgesics; however, in many cases, a more potent and effective polypharmacological approach is needed to promote clinically significant improvement. Additionally, considering side effects caused by current painkillers, drug discovery is once more turning to nature as a source of more efficient therapeutic alternatives. In this context, arthropod venoms contain a vast array of bioactive substances that have evolved to selectively bind to specific pharmacological targets involved in the pain signaling pathway, playing an important role as pain activators or modulators, the latter serving as promising analgesic agents. The current review explores how the pain pathway works and surveys neuroactive compounds obtained from arthropods' toxins, which function as pain modulators through their interaction with specific ion channels and membrane receptors, emerging as promising candidates for drug design and development.

Keywords: Acid-sensing ion channels; Glutamate; Purinergic receptors; Sodium channels; TRPV receptors; Voltage-dependent calcium channels.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Analgesics / pharmacology*
  • Animals
  • Arthropod Venoms / pharmacology*
  • Calcium Channels / drug effects
  • Calcium Channels / physiology
  • Humans
  • Pain / physiopathology
  • Signal Transduction / drug effects
  • Signal Transduction / physiology
  • Sodium Channels / drug effects
  • Sodium Channels / physiology
  • TRPV Cation Channels / drug effects
  • TRPV Cation Channels / physiology

Substances

  • Analgesics
  • Arthropod Venoms
  • Calcium Channels
  • Sodium Channels
  • TRPV Cation Channels
  • TRPV1 protein, human