鱼尼丁受体及以其为靶标的杀虫剂

Ryanodine receptor(RyR)and insecticides targeting RyR

作为最大的离子通道受体蛋白,鱼尼丁受体(Ry R)主要介导生物体胞内钙离子(Ca^(2+))释放而对肌肉兴奋-收缩耦联等生命活动起关键作用。由于在昆虫和脊椎动物体内存在显著差异,Ry R成为现代杀虫剂研发的理想靶标。由此开发的以氟苯虫酰胺和氯虫苯甲酰胺为代表的双酰胺类杀虫剂也成为最重要的杀虫剂品类之一。对Ry R及其Ca^(2+)释放通道的结构和功能进行介绍,并对以Ry R为靶标的杀虫剂(主要是双酰胺类杀虫剂)的研发背景与现状、化学合成、作用机制、生物活性、安全性、抗性、制剂及应用等进行总结,旨在为该类杀虫剂的研究、开发和应用提供指导。

As the largest ion channel receptor protein,Ryanodine Receptor(RyR)mainly mediates the release of Ca^(2+)from intracellular stores and hereby plays a crucial role in excitation-contraction coupling of muscle and other life activities in organisms.Because of its significant differences in insects and vertebrates,RyR is an ideal target for modern insecticide development.As a result of development on the insecticides targeting RyR,the diamide insecticides,represented by flubendiamide and chlorantraniliprole,have become one of the most important insecticide categories.In this paper,the structure and function of RyR and its Ca^(2+)release channel were introduced,and the research background and status quo,chemical synthesis,mechanism of action,biological activity,safety,resistance,formulation and application of the insecticides targeting RyR(mainly diamide insecticides)were summarized,aiming to provide a guidance for the research,development and application of this class of insecticides.