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- W3089544437 abstract "Abstract BACKGROUND Meta‐ diamides [3‐benzamido‐ N ‐(4‐(perfluoropropan‐2‐yl)phenyl)benzamides] show high insecticide activity by acting as antagonists to the insect resistance to dieldrin (RDL) γ‐aminobutyric acid (GABA) receptors. In contrast, low‐level antagonist activities of meta ‐diamides have been demonstrated against the human GABA type A receptor (GABA A R) α1β2γ2S, mammalian GABA A R α1β3γ2S, and the human glycine receptor (GlyR) α1β. Glycine residue 336 in the membrane‐spanning region M3 of the Drosophila RDL GABA receptor is essential for its high sensitivity to meta ‐diamide 7 , [3‐benzamido‐ N ‐(2‐bromo‐4‐(perfluoropropan‐2‐yl)‐6‐(trifluoromethyl)phenyl)‐2‐fluorobenzamide]. RESULTS We examined the effects of an equivalent mutation (M288G) in spontaneously opened human GABA A R β3 homomers using membrane potential assay. Picrotoxin and fipronil blocked spontaneously opened human GABA A Rs β3 and β3‐M286G in a concentration‐dependent manner. In contrast, meta ‐diamide 7 did not block spontaneously opened GABA A R β3 homomers, although meta ‐diamide 7 blocked spontaneously opened GABA A R β3‐M286G homomers. In addition, inhibitory potency of meta ‐diamide 7 for GABA‐induced membrane potential change in cells expressing GABA A R α1β3‐M286G was much higher than that in cells expressing GABA A R α1β3. In the same way, the equivalent mutation (A288G) in GlyR α1 increased the inhibitory potency of meta ‐diamide 7 for GlyRs α1 and α1β. CONCLUSION Studies substituting an equivalent mutation (M288G) in spontaneously opening human GABA A R β3 homomers and human GABA A Rs α1β3 heteromers suggest that M286 in human GABA A R β3 is important for the low sensitivity to meta ‐diamide 7 . In this study, we summarize the mechanisms underlying the selectivity of meta ‐diamides between insect RDL and human GABA and glycine receptors. © 2020 Society of Chemical Industry" @default.
- W3089544437 created "2020-10-08" @default.
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- W3089544437 date "2020-10-13" @default.
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- W3089544437 title "Mechanisms underlying the selectivity of <i>meta</i> ‐diamides between insect resistance to dieldrin ( <scp>RDL</scp> ) and human γ‐aminobutyric acid ( <scp>GABA</scp> ) and glycine receptors" @default.
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- W3089544437 doi "https://doi.org/10.1002/ps.6116" @default.
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