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Actions of imidacloprid, clothianidin and related neonicotinoids on nicotinic acetylcholine receptors of American cockroach neurons and their relationships with insecticidal potency

机译:吡虫啉,可尼丁和相关新烟碱类对美国蟑螂神经元烟碱乙酰胆碱受体的作用及其与杀虫力的关系

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摘要

The actions of neonicotinoid insecticides on nicotinic acetylcholine receptors (nAChRs) in the terminal abdominal ganglion neurons of the American cockroach were investigated using whole-cell patch-clamp electrophysiology. Neonicotinoids possessing a nitromethylene group showed higher agonist affinity than the corresponding nitroimine analogues, whereas compounds with an acyclic guanidine moiety showed greater agonist efficacy than the corresponding cyclic compounds. Imidacloprid showed the lowest agonist efficacy of all neonicotinoids and low concentrations of imidacloprid attenuated acetylcholine-induced currents. However, such blocking actions were minimal with other neonicotinoids. The diverse actions of neonicotinoids on nAChRs, combined with target accessibility based on hydrophobicity, appears to account for their insecticidal potency on cockroaches measured in the presence of metabolic inhibitors. © Pesticide Science Society of Japan.
机译:使用全细胞膜片钳电生理研究了新烟碱类杀虫剂对美洲蟑螂末端腹神经节神经元中烟碱乙酰胆碱受体(nAChRs)的作用。具有硝基亚甲基的新烟碱类化合物显示出比相应的硝基亚胺类似物更高的激动剂亲和力,而具有无环胍部分的化合物则显示出比相应的环状化合物更高的激动剂功效。吡虫啉显示出所有新烟碱类的激动剂功效最低,吡虫啉减毒乙酰胆碱诱导的电流浓度低。但是,其他新烟碱类药物的阻断作用极小。新烟碱类化合物对nAChRs的不同作用,加上基于疏水性的靶标可及性,似乎说明了它们在代谢抑制剂存在下对蟑螂的杀虫力。 ©日本农药学会。

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