Phenyl imidazolidin-2-ones antagonize a beta-adrenergic-like octopamine receptor in diamondback moth (Plutella xylostella)
文献类型： 外文期刊
作者： Deng, Xi-le 1 ; Guo, Lei 2 ; Ma, Hai-hao 1 ; Hu, Xue-ping 3 ; Zhou, Xiao-mao 1 ;
作者机构： 1.Hunan Acad Agr Sci, Inst Agr Biotechnol, Changsha 410125, Peoples R China
2.Zhejiang Univ, Inst Insect Sci, Minist Agr, Key Lab Mol Biol Crop Pathogens & Insects, Hangzhou, Peoples R China
3.Zhejiang Univ, Coll Pharmaceut Sci, Hangzhou, Peoples R China
关键词： octopamine receptor; Plutella xylostella; agonists; antagonists; gene expressions; Ca2+ concentration
期刊名称：PEST MANAGEMENT SCIENCE （ 影响因子：3.75； 五年影响因子：3.861 ）
ISSN： 1526-498X
年卷期：
页码：
收录情况： SCI
摘要： BACKGROUND The diamondback moth (Plutella xylostella) is one of the most destructive lepidopteran pests on cruciferous vegetables. However, resistance has emerged to current chemical and biological insecticides used for P. xylostella control, indicating the necessity of screening new targets on P. xylostella, and finding new insecticides against P. xylostella. In particular, octopamine receptors are representative G protein-coupled receptors found only in invertebrates and are potential targets for identifying novel insecticides. RESULTS A beta-adrenergic-like octopamine receptor gene (PxOA2B1) was cloned, and its pharmacological characteristics in P. xylostella were studied. The results demonstrated that octopamine could activate the PxOA2B1 receptor, with a half-maximal effective concentration (EC50) of 49.5 nm. Amitraz, an insecticide and acaricide, and its metabolite (N-2,4-dimethylphenyl-N '-methylformamidine; DPMF) were also found to act as PxOAB1R agonists. We synthesized phenyl imidazolidin-2-one derivatives 3a-h using DPMF as the lead compound, and compounds 3a-h showed similar antagonist activities as phentolamine, mianserin and chlorpromazine. In particular, 3d, with an EC50 of 25.2 nm, showed very similar antagonist activity to mianserin. CONCLUSION This research found that PxOAB1R might be a potential target for P. xylostella control. Phenyl imidazolidin-2-ones could be novel potential antagonists targeted at octopamine receptors and would be useful tools for the design and development of novel insecticides.
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