Insect-vertebrate chimeric nicotinic acetylcholine receptors identify a region, loop B to the N-terminus of the Drosophila Dalpha2 subunit, which contributes to neonicotinoid sensitivity

Neurosci Lett. 2005 Sep 9;385(2):168-72. doi: 10.1016/j.neulet.2005.05.014.

Abstract

A chimera based on the chicken alpha4 nicotinic acetylcholine receptor (nAChR) subunit containing an insert from loop B to the N-terminus of the Drosophila melanogaster Dalpha2 (=SAD) subunit was constructed and co-expressed with the chicken beta2 nAChR subunit in Xenopus laevis oocytes. The actions of the neonicotinoid insecticide imidacloprid were examined. Replacement of the region loop B to the N-terminus of the alpha4 subunit by the corresponding region of the Dalpha2 subunit had little effect on the concentration-response curve for imidacloprid. However, replacement of Glu219 by proline in the YXCC motif in loop C of the chimeric alpha4 subunit resulted in a marked displacement to the left of the concentration-response curve for imidacloprid not seen when an equivalent mutation was made in the alpha4beta2 nAChR. The results suggest that the region loop B to the N-terminus in the Dalpha2 subunit contributes to the high imidacloprid sensitivity of the hybrid Dalpha2beta2 nAChR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Motifs / physiology
  • Amino Acid Sequence / physiology
  • Amino Acid Substitution / physiology
  • Animals
  • Chickens
  • Cholinergic Agents / pharmacology
  • Drosophila melanogaster / genetics
  • Drosophila melanogaster / metabolism*
  • Drug Resistance / genetics
  • Imidazoles / pharmacology*
  • Neonicotinoids
  • Nitro Compounds
  • Oocytes
  • Protein Structure, Tertiary / physiology
  • Protein Subunits / chemistry*
  • Protein Subunits / drug effects
  • Protein Subunits / genetics
  • Receptors, Nicotinic / chemistry*
  • Receptors, Nicotinic / drug effects
  • Receptors, Nicotinic / genetics
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / drug effects
  • Recombinant Fusion Proteins / genetics
  • Xenopus laevis

Substances

  • Cholinergic Agents
  • Imidazoles
  • Neonicotinoids
  • Nitro Compounds
  • Protein Subunits
  • Receptors, Nicotinic
  • Recombinant Fusion Proteins
  • imidacloprid