Insecticidal activity and nicotinic acetylcholine receptor binding of dinotefuran and its analogues in the housefly, Musca domestica

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 [I-125]alpha-bungarotoxin ([I-125]alpha-BGTX) and [H-3]imidacloprid ([H-3]IMI) as radioligands. The activity of some selected compounds measured with [H-3]IMI was 10(4)-fold higher than that measured with [I-125]alpha-BGTX. With [H-3]IMI as a radioligand, dinotefuran was 13-fold less active than imidacloprid. The inhibitory effect of dinotefuran on the binding of [H-3]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 [H-3]IMI showed that the higher the binding activity, the higher was the insecticidal activity. (C) 2003 Society of Chemical Industry.