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最近发现了一类新型二酰胺类杀虫剂——氟虫酰胺和氯虫酰胺,其作用靶标是鱼尼丁受体(ryanodine receptors,RyRs)。本文对RyR的结构与功能、电压门控钙离子通道和鱼尼丁受体钙离子释放通道对细胞质钙离子内环境稳定的调节以及二酰胺类杀虫剂对RyRs作用的分子机理进行综述。二酰胺类杀虫剂使昆虫RyR通道处于持续的开放状态,引发钙离子从肌质网腔内大量释放,破坏了细胞质钙离子内环境的稳定,从而产生不同的药物学特性。这些变化都是由一个不同于鱼尼丁在RyR上的结合部位介导的。该类杀虫剂的作用对昆虫RyRs是高度专一的,结果产生选择毒性。由于二酰胺类杀虫剂的结构独特,作用方式新颖,对鳞翅目害虫效果好、杀虫谱广,对各种益虫和天敌安全,并对现用的杀虫剂无交互抗性,故它们非常适合于抗性治理和IPM。
Recently, a new class of diamide insecticides, flubendiamide and chlorantraniliprole, have been discovered that target ryanodine receptors (RyRs). This review summarizes the structure and function of RyR, the regulation of voltage-gated Ca2 + channels and the regulation of the intracellular Ca2 + homeostasis by calcium channel in dunedin receptor, and the molecular mechanism of RyRs by diamide insecticides. Diamide insecticides keep the insect RyR channel in a sustained open state, triggering a large release of calcium ions from the sarcoplasmic reticulum, disrupting the stability of the cytoplasmic calcium ion environment and resulting in different pharmacological properties. These changes are mediated by a different binding site to the RyR on the RyR. The insecticide’s action on insect RyRs is highly specific, resulting in selective toxicity. Because of the unique structure of diamide pesticides, new mode of action, good effect on lepidopteran pests, broad insecticidal spectrum, safe for all kinds of beneficial insects and natural enemies, and no cross-resistance to the existing pesticides They are ideally suited for resistance management and IPM.