Spalthoff Christian, Salgado Vincent L, Balu Narayanan, David Michael D, Hehlert Philip, Huang Huazhang, Jones John E, Kandasamy Ramani, Knudsen Gabriel A, Lelito Katherine R, Machamer James B, Nesterov Alexandre, Tomalski Michael, Wahl Gregory D, Wedel Barbara J, Göpfert Martin C
Department of Cellular Neurobiology, University of Göttingen, Göttingen, Germany.
BASF Corp, Research Triangle Park, NC, USA.
Pest Manag Sci. 2023 May;79(5):1635-1649. doi: 10.1002/ps.7352. Epub 2023 Mar 1.
Pyridazine pyrazolecarboxamides (PPCs) are a novel insecticide class discovered and optimized at BASF. Dimpropyridaz is the first PPC to be submitted for registration and controls many aphid species as well as whiteflies and other piercing-sucking insects.
Dimpropyridaz and other tertiary amide PPCs are proinsecticides that are converted in vivo into secondary amide active forms by N-dealkylation. Active secondary amide metabolites of PPCs potently inhibit the function of insect chordotonal neurons. Unlike Group 9 and 29 insecticides, which hyperactivate chordotonal neurons and increase Ca levels, active metabolites of PPCs silence chordotonal neurons and decrease intracellular Ca levels. Whereas the effects of Group 9 and 29 insecticides require TRPV (Transient Receptor Potential Vanilloid) channels, PPCs act in a TRPV-independent fashion, without compromising cellular responses to Group 9 and 29 insecticides, placing the molecular PPC target upstream of TRPVs.
PPCs are a new class of chordotonal organ modulator insecticide for control of piercing-sucking pests. Dimpropyridaz is a PPC proinsecticide that is activated in target insects to secondary amide forms that inhibit the firing of chordotonal organs. The inhibition occurs at a site upstream of TRPVs and is TRPV-independent, providing a novel mode of action for resistance management. © 2023 BASF Corporation. Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.
哒嗪吡唑甲酰胺（PPCs）是巴斯夫公司发现并优化的一类新型杀虫剂。丁丙哒螨灵是首个提交登记申请的PPC，可防治多种蚜虫以及粉虱和其他刺吸式昆虫。
丁丙哒螨灵和其他叔酰胺类PPC是前体杀虫剂，在体内通过N - 脱烷基作用转化为仲酰胺活性形式。PPC的活性仲酰胺代谢物能有效抑制昆虫弦音感受器神经元的功能。与第9组和第29组杀虫剂不同，第9组和第29组杀虫剂会使弦音感受器神经元过度激活并增加钙离子水平，而PPC的活性代谢物会使弦音感受器神经元沉默并降低细胞内钙离子水平。第9组和第29组杀虫剂的作用需要瞬时受体电位香草酸（TRPV）通道介导，而PPC以不依赖TRPV的方式起作用，且不影响细胞对第9组和第29组杀虫剂的反应，这表明PPC的分子靶点位于TRPV上游。
PPC是一类新型的用于防治刺吸式害虫的弦音感受器器官调节剂杀虫剂。丁丙哒螨灵是一种PPC前体杀虫剂，在靶标昆虫体内被激活为仲酰胺形式，抑制弦音感受器器官的放电。这种抑制作用发生在TRPV上游的位点，且不依赖TRPV，为抗性治理提供了一种新的作用模式。© 2023巴斯夫公司。《害虫管理科学》由约翰·威利父子有限公司代表化学工业协会出版。
