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The mode of action of isocycloseram: A novel isoxazoline insecticide
Pesticide Biochemistry and Physiology ( IF 4.2 ) Pub Date : 2022-08-25 , DOI: 10.1016/j.pestbp.2022.105217
Judith Blythe 1 , Fergus G P Earley 1 , Katarzyna Piekarska-Hack 1 , Lucy Firth 1 , Julia Bristow 1 , Elizabeth A Hirst 1 , James A Goodchild 1 , Elke Hillesheim 2 , Andrew J Crossthwaite 1
Affiliation  

Isocycloseram is a novel isoxazoline insecticide and acaricide with activity against lepidopteran, hemipteran, coleopteran, thysanopteran and dipteran pest species. Isocycloseram selectively targets the invertebrate Rdl GABA receptor at a site that is distinct to fiproles and organochlorines. The widely distributed cyclodiene resistance mutation, A301S, does not affect sensitivity to isocycloseram, either in vitro or in vivo, demonstrating the suitability of isocylsoseram to control pest infestations with this resistance mechanism. Detailed studies demonstrated that the binding sites relevant to the insecticidal activity of avermectins and isocycloseram are distinct. Isocycloseram was shown to compete for binding with metadiamide insecticides related to broflanilide. In addition, a G335M mutation in the third transmembrane domain of the Rdl GABA receptor, impaired the ability of both isocycloseram and metadiamides to block the GABA mediated response. As such the Insecticides Resistance Action Committee (IRAC) has classified isocycloseram in Group 30 “GABA-Gated Chloride Channel Allosteric Modulators”.



中文翻译:

异环血清的作用方式:一种新型异恶唑啉杀虫剂

Isocycloseram 是一种新型异恶唑啉杀虫剂和杀螨剂,对鳞翅目、半翅目、鞘翅目、缨翅目和双翅目害虫物种具有活性。Isocycloseram 选择性地靶向无脊椎动物 Rdl GABA 受体,该受体位于与 fiproles 和有机氯不同的位点。广泛分布的环二烯抗性突变 A301S 在体外或体内均不影响对异环血清的敏感性,表明异环血清适用于控制具有这种抗性机制的害虫侵扰。详细研究表明,与阿维菌素和异环血清的杀虫活性相关的结合位点是不同的。Isocycloseram 被证明可以与与溴苯胺相关的间二酰胺类杀虫剂竞争结合。此外,Rdl GABA 受体的第三个跨膜结构域中的 G335M 突变削弱了异环血清和间二酰胺阻断 GABA 介导的反应的能力。因此,杀虫剂抗性行动委员会 (IRAC) 已将异环血清归入第 30 组“GABA-门控氯离子通道变构调节剂”。

更新日期:2022-08-27
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