The binding properties of cycloxaprid on insect native nAChRs partially explain the low cross‐resistance with imidacloprid in Nilaparvata lugens

BACKGROUND Neonicotinoids, such as imidacloprid, are selective agonists of insect nicotinic acetylcholine receptors (nAChRs) used to control Nilaparvata lugens, a major rice insect pest. High imidacloprid resistance has been reported in N. lugens both in the laboratory and in the field. Cycloxaprid (CYC), an oxa‐bridged cis‐nitromethylene neonicotinoid, showed high insecticidal activity against N. lugens and low cross‐resistance in imidacloprid‐resistant strains and field populations. RESULTS Binding studies demonstrated that imidacloprid has two binding sites with different affinities (Kd = 3.18 ± 0.43 pm and 1.78 ± 0.19 nm) in N. lugens nAChRs. CYC was poor at displacing [3H]imidacloprid at its high‐affinity binding site (Ki = 159.38 ± 20.43 nm), but quite efficient at the low‐affinity binding site (Ki = 1.27 ± 0.35 nm). These data showed that CYC had overlapping binding sites with imidacloprid only at its low‐affinity binding site. Therefore, the low displacement ability of CYC against imidacloprid binding at its high‐affinity site could partially explain the low cross‐resistance of CYC in imidacloprid‐resistant populations. CONCLUSION The high insecticidal activity, low cross‐resistance and different binding properties on insect nAChRs of CYC show that it is a potential insecticide for the control of N. lugens and related insect pests, especially ones with high resistance to neonicotinoids.