Characterization of a nicotinic acetylcholine receptor binding site for sulfoxaflor, a new sulfoximine insecticide for the control of sap-feeding insect pests

Sulfoxaflor (SFX, Isoclast (TM) Active) is a recently developed sulfoximine insecticide that is highly effective against sap-feeding insect pests. SFX has been shown to act through an interaction with insect nicotinic acetylcholine receptors (nAChRs). SFX was previously found to interact weakly with the binding site for the neonicotinoid imidacloprid. However, radioligand displacement studies characterizing the binding site of the insecticide SFX itself have not been conducted. In this study, we report the characterization of a high affinity [H-3]SFX Myzus persicae (green peach aphid, GPA) binding site with relatively low abundance. Through the evaluation of a set of SFX analogs, we have demonstrated that displacement of [H-3]SFX shows an excellent correlation with GPA toxicity, and thus is toxicologically relevant. Comparison with the previously described methyl-SFX binding site information reveals differences with the SFX binding site that are discussed herein. [H-3]SFX therefore represents a new tool for the characterization of insect nAChRs.