Super agonist actions of clothianidin and related compounds on the SAD beta 2 nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes.
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.
Ihara
Makoto
M
Graduate School of Agriculture, Kinki University, Nakamachi, Nara, Japan.
Matsuda
Kazuhiko
K
Shimomura
Masaru
M
Sattelle
David B
DB
Komai
Koichiro
K
D000109:Acetylcholine / Q000494:pharmacology; D000691:Anabasine / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D018076:DNA, Complementary / Q000235:genetics; D004274:DNA, Recombinant / Q000235:genetics; D029721:Drosophila Proteins; D004594:Electrophysiology / Q000379:methods; D006146:Guanidines / Q000737:chemistry* / Q000494:pharmacology*; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D000073943:Neonicotinoids; D018722:Nicotinic Agonists / Q000737:chemistry* / Q000494:pharmacology*; D009574:Nitro Compounds; D009865:Oocytes / Q000187:drug effects / Q000378:metabolism; D011978:Receptors, Nicotinic / Q000187:drug effects* / Q000235:genetics / Q000502:physiology; D013844:Thiazoles; D014162:Transfection; D014982:Xenopus laevis
D000109:Acetylcholine; D000691:Anabasine; D018076:DNA, Complementary; D004274:DNA, Recombinant; D029721:Drosophila Proteins; D006146:Guanidines; D007093:Imidazoles; D000073943:Neonicotinoids; D018722:Nicotinic Agonists; D009574:Nitro Compounds; D011978:Receptors, Nicotinic; D013844:Thiazoles; C113681:nicotinic acetylcholine receptor alpha-subunits, Drosophila; C480342:clothianidin; C082359:imidacloprid