Super agonist actions of clothianidin and related compounds on the SAD beta 2 nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes

Biosci Biotechnol Biochem. 2004 Mar;68(3):761-3. doi: 10.1271/bbb.68.761.

Abstract

To compare the actions of clothianidin, a neonicotinoid acting on insect nicotinic acetylcholine receptors, and related compounds with that of imidacloprid, the compounds were tested on the Drosophila SAD-chicken beta2 nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes using two-electrode voltage-clamp electrophysiology. The maximum response of the SAD beta 2 nicotinic receptor to clothianidin was larger than that observed for acetylcholine. Ring breakage of the imidazolidine ring of imidacloprid resulting in the generation of a guanidine group was critical for this super agonist action.

MeSH terms

  • Acetylcholine / pharmacology
  • Anabasine / analogs & derivatives
  • Anabasine / chemistry
  • Anabasine / pharmacology
  • Animals
  • DNA, Complementary / genetics
  • DNA, Recombinant / genetics
  • Drosophila Proteins
  • Electrophysiology / methods
  • Guanidines / chemistry*
  • Guanidines / pharmacology*
  • Imidazoles / chemistry
  • Imidazoles / pharmacology
  • Molecular Structure
  • Neonicotinoids
  • Nicotinic Agonists / chemistry*
  • Nicotinic Agonists / pharmacology*
  • Nitro Compounds
  • Oocytes / drug effects
  • Oocytes / metabolism
  • Receptors, Nicotinic / drug effects*
  • Receptors, Nicotinic / genetics
  • Receptors, Nicotinic / physiology
  • Thiazoles
  • Transfection
  • Xenopus laevis

Substances

  • DNA, Complementary
  • DNA, Recombinant
  • Drosophila Proteins
  • Guanidines
  • Imidazoles
  • Neonicotinoids
  • Nicotinic Agonists
  • Nitro Compounds
  • Receptors, Nicotinic
  • Thiazoles
  • nicotinic acetylcholine receptor alpha-subunits, Drosophila
  • nicotinic receptor beta2
  • clothianidin
  • imidacloprid
  • Anabasine
  • Acetylcholine