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首页> 外文期刊>Journal of Agricultural and Food Chemistry >Radioligand Recognition of Insecticide Targets
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Radioligand Recognition of Insecticide Targets

机译：放射性配体识别杀虫剂靶标

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摘要

Insecticide radioligands allow the direct recognition and analysis of the targets and mechanisms of toxic action critical to effective and safe pest control. These radioligands are either the insecticides themselves or analogs that bind at the same or coupled sites. Preferred radioligands and their targets, often in both insects and mammals, are trioxabicyclooctanes for the gamma-aminobutyric acid (GABA) receptor, avermectin for the glutamate receptor, imidadoprid for the nicotinic receptor, ryanodine and chlorantrarnliprole for the ryanodine receptor, and rotenone or pyridaben for NADH(+) ubiquinone oxidoreductase. Pyrethroids and other Na+ channel modulator insecticides are generally poor radioligands due to lipophilicity and high nonspecific binding. For target site validation, the structure activity relationships competing with the radioligand in the binding assays should be the same as that for insecticidal activity or toxicity except for rapidly detoxified or proinsecticide analogs. Once the radioligand assay is validated for relevance, it will often help define target site modifications on selection of resistant pest strains, selectivity between insects and mammals, and interaction with antidotes and other chemicals at modulator sites. Binding assays also serve for receptor isolation and photoaffinity labeling to characterize the interactions involved.
机译：杀虫剂放射性配体允许直接识别和分析对有效和安全的害虫控制至关重要的毒性作用的目标和机制。这些放射性配体是杀虫剂本身或类似物在相​​同或偶联位点结合的类似物。通常在昆虫和哺乳动物中的优选放射性配体及其靶标是γ-氨基丁酸（GABA）受体，谷氨酸受体的Avermectin，硝基氨基受体，柠檬籽和氯苯的氨基丙二酰亚胺蛋白，柠檬胺受体，以及Rotenone或Pyridaben的丙二酰亚胺蛋白对于NADH（+）泛醌氧化还原酶。拟除虫菊酯和其他Na +通道调节剂杀虫剂通常由于亲脂性和高的非特异性结合而导致的放射性配体差。对于靶位验证，结合测定中与放射性配体竞争的结构活性关系应与杀虫活性或毒性相同，除了快速解毒或不孤立的类别类似物。一旦放射性配体测定被验证了相关性，它通常会有助于确定对抗性害虫菌株的选择，昆虫和哺乳动物的选择性的靶位修饰，以及与调节位点的反相和其他化学物质。结合测定还用于受体分离和光化素位标记，以表征所涉及的相互作用。

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