title: Insecticidal activity and nicotinic acetylcholine receptor binding of dinotefuran and its analogues in the housefly, Musca domestica.
abstract: The insecticidal activity of dinotefuran and 23 related compounds against the housefly, Musca domestica (L) was measured by injection with metabolic inhibitors. Dinotefuran was less active than imidacloprid and clothianidin by a factor of 10 in molar concentrations. Their binding activities to the fly-head membrane preparation were measured by using [125I]alpha-bungarotoxin ([125I]alpha-BGTX) and [3H]imidacloprid ([3H]IMI) as radioligands. The activity of some selected compounds measured with [3H]IMI was 10(4)-fold higher than that measured with [125I]alpha-BGTX. With [3H]IMI as a radioligand, dinotefuran was 13-fold less active than imidacloprid. The inhibitory effect of dinotefuran on the binding of [3H]IMI to the membrane preparation was in a competitive manner. Quantitative analysis of the insecticidal activity of the test compounds with the binding activity measured with [3H]IMI showed that the higher the binding activity, the higher was the insecticidal activity.
authors.affiliation: Research Institute for Advanced Science and Technology, Osaka Prefecture University, Sakai, Osaka 599-8570, Japan.
authors.forename: Kazuhisa
authors.initials: K
authors.lastname: Kiriyama
authors.forename: Hisashi
authors.initials: H
authors.lastname: Nishiwaki
authors.forename: Yoshiaki
authors.initials: Y
authors.lastname: Nakagawa
authors.forename: Keiichiro
authors.initials: K
authors.lastname: Nishimura
mesh_terms: D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002038:Bungarotoxins / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity; D005260:Female; D006146:Guanidines / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity*; D006793:Houseflies / Q000187:drug effects* / Q000378:metabolism; D007093:Imidazoles / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity; D007306:Insecticides / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity*; D007457:Iodine Radioisotopes; D008954:Models, Biological; D000073943:Neonicotinoids; D009574:Nitro Compounds / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity*; D011978:Receptors, Nicotinic / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014316:Tritium
chemical_list: D002038:Bungarotoxins; D006146:Guanidines; D007093:Imidazoles; D007306:Insecticides; D007457:Iodine Radioisotopes; D000073943:Neonicotinoids; D009574:Nitro Compounds; D011978:Receptors, Nicotinic; D014316:Tritium; C465368:dinotefuran; C082359:imidacloprid