Emodepside and SL0-1 potassium channels: a review

Exp Parasitol. 2012 Sep;132(1):40-6. doi: 10.1016/j.exppara.2011.08.012. Epub 2011 Sep 3.

Abstract

Nematode parasites infect humans and domestic animals; treatment and prophylaxis require anthelmintic drugs because vaccination and sanitation is limited. Emodepside is a more recently introduced cyclooctadepsipeptide drug that has actions against GI nematodes, lungworm, and microfilaria. It has a novel mode of action which breaks resistance to the classical anthelmintics (benzimidazoles, macrocyclic lactones and cholinergic agonists). Here we review studies on its mode of action which suggest that it acts to inhibit neuronal and muscle activity of nematodes by increasing the opening of calcium-activated potassium (SLO-1) channels.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Anthelmintics / pharmacology*
  • Anthelmintics / therapeutic use
  • Caenorhabditis elegans / drug effects
  • Caenorhabditis elegans / metabolism
  • Caenorhabditis elegans / physiology
  • Depsipeptides / pharmacology*
  • Depsipeptides / therapeutic use
  • Drug Resistance
  • Humans
  • Large-Conductance Calcium-Activated Potassium Channels / drug effects*
  • Large-Conductance Calcium-Activated Potassium Channels / metabolism
  • Membrane Potentials / drug effects
  • Membrane Potentials / physiology
  • Muscle Contraction / drug effects
  • Muscle Contraction / physiology
  • Nematoda / drug effects*
  • Nematoda / metabolism
  • Nematoda / physiology
  • Nematode Infections / drug therapy*
  • Nematode Infections / parasitology
  • Nematode Infections / prevention & control
  • Neuromuscular Junction / drug effects
  • Neuromuscular Junction / metabolism
  • Neuropeptides / metabolism
  • Receptors, Peptide / drug effects
  • Receptors, Peptide / metabolism

Substances

  • Anthelmintics
  • Depsipeptides
  • Large-Conductance Calcium-Activated Potassium Channels
  • Neuropeptides
  • Receptors, Peptide
  • alpha-latrotoxin receptor
  • emodepside