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A comparison of the modes of action of novel meta-diamide insecticides and conventional noncompetitive antagonists on the Spodoptera litura RDL GABA receptor

机译:新型间二酰胺类杀虫剂和常规非竞争性拮抗剂对斜纹夜蛾RDL GABA受体作用方式的比较

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摘要

Novel meta-diamides [3-benzamido-N-(4-(perfluoropropan-2-yl)phenyl)benzaniides] are a distinct class of RDL GABA receptor antagonists with high larvicidal activity against Spodoptera litura. Genotyping showed that the S. litura RDL GABA receptor subunit (SL-RDL) gene had Ser at its 2' position, which was widely distributed among field S. litura larvae in Japan. We investigated the modes of action of meta-diamides on SL-RDLbd homomers using a membrane potential assay. S2'N and T6'V mutations had profound effects on the inhibitory activities of fipronil and α-endosulfan, whereas these mutations had no effect on the inhibitory activities of meta-diamides. In contrast, a G319M mutation abolished the inhibitory activities of meta-diamides, whereas it had only a small effect on the activities of fipronil and a-endosulfan. These results suggest that the site of action of meta-diamides is near G319 in the third transmembrane segment of SL-RDL homomers, which is distinct from those of fipronil and a-endosulfan.
机译:新型间二酰胺[3-苯甲酰胺基-N-(4-(全氟丙烷-2-基)苯基)苯甲腈]是一类独特的RDL GABA受体拮抗剂,对斜纹夜蛾具有高杀幼虫活性。基因分型表明,斜纹夜蛾RDL GABA受体亚基(SL-RDL)基因的Ser位于其2'端,在日本田间斜纹夜蛾幼虫中广泛分布。我们使用膜电位测定法研究了偏二酰胺对SL-RDLbd同聚物的作用方式。 S2'N和T6'V突变对氟虫腈和α-硫丹的抑制活性有深远影响,而这些突变对间二酰胺的抑制活性无影响。相反,G319M突变取消了对间二酰胺的抑制活性,而对氟虫腈和α-硫丹的活性影响很小。这些结果表明,间二酰胺的作用位点在SL-RDL同聚物的第三跨膜区段中的G319附近,这不同于氟虫腈和α-硫丹。

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