A single amino acid change makes a rat neuronal sodium channel highly sensitive to pyrethroid insecticides

FEBS Lett. 2000 Mar 24;470(2):135-8. doi: 10.1016/s0014-5793(00)01305-3.

Abstract

Two amino acid substitutions in a housefly sodium channel, L1014F in domain IIS6 and M918T in the IIS4-S5 linker, have been identified in kdr and super-kdr pyrethroid-resistant phenotypes, respectively. Unlike their native insect counterparts, mammalian sodium channels are only weakly sensitive to pyrethroids. Do the sodium channels of mammal and pyrethroid-resistant housefly share similar structural characteristics that account for their low pyrethroid sensitivities? We report here that substitution of isoleucine for methionine at position 874 (equivalent to the super-kdr site 918 in the housefly) in the rat IIA alpha-subunit causes a 100-fold increase in sensitivity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Amino Acid Substitution / genetics*
  • Animals
  • Brain
  • Drug Resistance / genetics
  • Electric Conductivity
  • Insecticides / metabolism
  • Insecticides / pharmacology*
  • Isoleucine / genetics
  • Molecular Sequence Data
  • Nitriles
  • Oocytes
  • Phenotype
  • Pyrethrins / metabolism
  • Pyrethrins / pharmacology*
  • Rats
  • Sequence Alignment
  • Sodium Channel Blockers*
  • Sodium Channels / chemistry
  • Sodium Channels / genetics
  • Sodium Channels / metabolism*
  • Xenopus laevis

Substances

  • Insecticides
  • Nitriles
  • Pyrethrins
  • Sodium Channel Blockers
  • Sodium Channels
  • Isoleucine
  • decamethrin