Overview of the Status and Global Strategy for Neonicotinoids

TLDR

Neonicotinoid insecticides, the fastest growing class in modern crop protection, selectively target insect nicotinic acetylcholine receptors and represent a milestone in insecticide research. The crystal structure of acetylcholine‑binding proteins underpins homology modeling of nAChR ligand‑binding domains, enabling virtual screening and rational design of novel insecticides. Because of their high target specificity, low non‑target risk, and versatile application, neonicotinoids remain essential for global integrated pest management and resistance programs, with life‑cycle management and generic products cementing their market dominance.

Abstract

In recent years, neonicotinoid insecticides have been the fastest growing class of insecticides in modern crop protection, with widespread use against a broad spectrum of sucking and certain chewing pests. As potent agonists, they act selectively on insect nicotinic acetylcholine receptors (nAChRs), their molecular target site. The discovery of neonicotinoids can be considered as a milestone in insecticide research and greatly facilitates the understanding of functional properties of the insect nAChRs. In this context, the crystal structure of the acetylcholine-binding proteins provides the theoretical foundation for designing homology models of the corresponding receptor ligand binding domains within the nAChRs, a useful basis for virtual screening of chemical libraries and rational design of novel insecticides acting on these practically relevant channels. Because of the relatively low risk for nontarget organisms and the environment, the high target specificity of neonicotinoid insecticides, and their versatility in application methods, this important class has to be maintained globally for integrated pest management strategies and insect resistance management programs. Innovative concepts for life-cycle management, jointly with the introduction of generic products, have made neonicotinoids the most important chemical class for the insecticide market.