Glutamate-activated chloride channels: Unique fipronil targets present in insects but not in mammals

Toshio Narahashi*, Xilong Zhao, Tomoko Ikeda, Vincent L. Salgado, Jay Z. Yeh

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

74 Scopus citations

Abstract

Selectivity to insects over mammals is one of the important characteristics for a chemical to become a useful insecticide. Fipronil was found to block cockroach GABA receptors more potently than rat GABA A receptors. Furthermore, glutamate-activated chloride channels (GluCls), which are present in cockroaches but not in mammals, were very sensitive to the blocking action of fipronil. The IC 50s of fipronil block were 30nM in cockroach GABA receptors and 1600nM in rat GABA A receptors. Moreover, GluCls of cockroach neurons had low IC 50s for fipronil. Two types of glutamate-induced chloride current were observed: desensitizing and non-desensitizing, with fipronil IC 50s of 800 and 10nM, respectively. We have developed methods to separately record these two types of GluCls. The non-desensitizing and desensitizing currents were selectively inhibited by trypsin and polyvinylpyrrolidone, respectively. In conclusion, in addition to GABA receptors, GluCls play a crucial role in selectivity of fipronil to insects over mammals. GluCls form the basis for development of selective and safe insecticides.

Original languageEnglish (US)
Pages (from-to)149-152
Number of pages4
JournalPesticide Biochemistry and Physiology
Volume97
Issue number2
DOIs
StatePublished - Jun 2010

Keywords

  • Cockroach neuron
  • Fipronil
  • GABA receptor
  • Glutamate-activated chloride channel
  • Polyvinylpyrrolidone
  • Rat neuron
  • Trypsin

ASJC Scopus subject areas

  • Agronomy and Crop Science
  • Health, Toxicology and Mutagenesis

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