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 showed that the mode of action of the meta-diamides was distinct from that of conventional noncompetitive antagonists (NCAs). The A2'S�T6'V mutation almost abolished the inhibitory effects of NCAs. However, meta-diamides inhibited the A2'S�T6'V mutant receptor at the same level as its activity with the wild-type receptor. In contrast, a G336M mutation in the third transmembrane domain of the Drosophila RDL GABA receptor abolished the inhibitory activities of meta-diamides, although the G336M mutation had little effect on the inhibitory activities of conventional NCAs. Molecular modeling studies also suggested that the binding site of meta-diamides was the transmembrane inter-subunit pocket near G336 of the Drosophila RDL GABA receptor, which was different from those of NCAs.

Comparison of the modes of action of novel meta-diamide insecticides and conventional noncompetitive antagonists on the RDL GABA receptor

248th National Meeting (2014)

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