Novel meta-diamides [3-benzamido-N-(4-(perfluoropropan-2-yl)phenyl)benzamides] are a distinct class of RDL GABA receptor antagonists with high larvicidal activity against Spodoptera litura. A membrane potential assay using wild type and mutant Drosophila RDL GABA receptors suggested that G336 in M3 of the Drosophila RDL GABA receptor was important for binding of meta-diamides and macrocyclic lactones. However, macrocyclic lactones, ivermectin and milbemectin, acted as agonists on wild-type Drosophila RDL GABA receptor. Molecular modeling studies revealed that meta-diamides bound to the inter-subunit pocket near G336 in the Drosophila RDL GABA receptor better when in the closed state than when in the open state. In contrast, macrocyclic lactones were revealed to bind to the Drosophila RDL GABA receptor when in the open state. This suggests that the actions and modes of binding meta-diamides to wild-type Drosophila RDL GABA receptor are different from those of macrocyclic lactones.

Comparison of the modes of action of novel meta-diamide insecticides and macrocyclic lactone insecticides on the RDL GABA receptor

248th National Meeting (2014)

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