The second generation of GABA receptor (GABA-R) antagonist insecticides consisting of isoxazolines (isox) and meta-diamides (m-DA) (Figure) is characterized by little or no cross resistance with the first generation (dieldrin, endosulfan, fipronil) and low potency at mammalian GABA-Rs. Binding site assays with [3H]EBOB, [3H]flualaner, [3H]m-DA and [3H]ivermectin (Ive) using Musca brain or Drosophila expressed RDL GABA-R establish close coupling (nM IC50 levels) between at least three unique sites. Models of Drosophila RDL GABA-R are used to elucidate the binding site interactions for EBOB, isox, m-DA and Ive. The second generation antagonists have rekindled excitement in the GABAergic insecticide area.Figure : Second generation GABA-R antagonist radioligandsStudies by:  J. E. Casida, K. Hirase, T. Iig, T. Nakao, Y. Ozoe, C. Zhao and colleagues.

Insecticide targets in insect GABA receptors: Binding sites for first and second generation antagonists and avermectin modulators

248th National Meeting (2014)

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