Identification of a Drosophila melanogaster glutamate-gated chloride channel sensitive to the antiparasitic agent avermectin

J Biol Chem. 1996 Aug 16;271(33):20187-91. doi: 10.1074/jbc.271.33.20187.

Abstract

Glutamate-gated chloride channels, members of the ligand-gated ion channel superfamily, have been shown in nematodes and in insects to be a target of the antiparasitic agent avermectin. Two subunits of the Caenorhabditis elegans glutamate-gated chloride channel have been cloned: GluCl-alpha and GluCl-beta. We report the cloning of a Drosophila melanogaster glutamate-gated chloride channel, DrosGluCl-alpha, which shares 48% amino acid and 60% nucleotide identity with the C. elegans GluCl channels. Expression of DrosGluCl-alpha in Xenopus oocytes produces a homomeric chloride channel that is gated by both glutamate and avermectin. The DrosGluCl-alpha channel has several unique characteristics not observed in C. elegans GluCl: dual gating by avermectin and glutamate, a rapidly desensitizing glutamate response, and a lack of potentiation of the glutamate response by avermectin. The pharmacological data support the hypothesis that the DrosGluCl-alpha channel represents the arthropod H-receptor and an important target for the avermectin class of insecticides.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Base Sequence
  • Chloride Channel Agonists*
  • Chloride Channels / genetics
  • DNA Primers / chemistry
  • Drosophila melanogaster / physiology*
  • Electric Conductivity
  • Excitatory Amino Acid Agonists / pharmacology*
  • Gene Expression
  • Genes, Insect*
  • Glutamates / physiology*
  • Ion Channel Gating / drug effects*
  • Ivermectin / analogs & derivatives*
  • Ivermectin / pharmacology
  • Molecular Sequence Data
  • RNA, Messenger / genetics
  • Receptors, Glutamate / physiology*
  • Sequence Alignment
  • Sequence Homology, Amino Acid
  • Xenopus laevis

Substances

  • Chloride Channel Agonists
  • Chloride Channels
  • DNA Primers
  • Excitatory Amino Acid Agonists
  • Glutamates
  • RNA, Messenger
  • Receptors, Glutamate
  • Ivermectin
  • avermectin

Associated data

  • GENBANK/U58776