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研究噻虫砜的作用模式:一种第四代新烟碱类杀虫剂。

Investigating the mode of action of sulfoxaflor: a fourth-generation neonicotinoid.

机构信息

Syngenta Crop Protection, Biological Sciences, Jealott's Hill International Research Centre, Bracknell, UK.

出版信息

Pest Manag Sci. 2013 May;69(5):607-19. doi: 10.1002/ps.3413. Epub 2012 Oct 30.

DOI:10.1002/ps.3413
PMID:23112103
Abstract

BACKGROUND

The precise mode of action of sulfoxaflor, a new nicotinic acetylcholine receptor-modulating insecticide, is unclear. A detailed understanding of the mode of action, especially in relation to the neonicotinoids, is essential for recommending effective pest management practices.

RESULTS

Radiolabel binding experiments using a tritiated analogue of sulfoxaflor ([(3) H]-methyl-SFX) performed on membranes from Myzus persicae demonstrate that sulfoxaflor interacts specifically with the high-affinity imidacloprid binding site present in a subpopulation of the total nAChR pool. In competition studies, imidacloprid-like neonicotinoids displace [(3) H]-methyl-SFX at pM concentrations. The effects of sulfoxaflor on the exposed aphid nervous system in situ are analogous to those of imidacloprid and nitenpyram, and finally the high-affinity sulfoxaflor binding site is absent in a Myzus persicae strain (clone FRC) possessing a single amino acid point mutation (R81T) in the β-nAChR, a region critical for neonicotinoid interaction.

CONCLUSION

The nicotinic acetylcholine receptor pharmacological profile of sulfoxaflor in aphids is consistent with that of imidacloprid. Additionally, the insecticidal activity of sulfoxaflor and the current commercialised neonicotinoids is affected by the point mutation in FRC Myzus persicae. Therefore, it is suggested that sulfoxalfor be considered a neonicotinoid, and that this be taken into account when recommending insecticide rotation partnering for effective resistance management programmes.

摘要

背景

新烟碱类杀虫剂噻虫砜的作用模式尚不清楚。详细了解其作用模式,尤其是与新烟碱类杀虫剂的关系,对于推荐有效的害虫管理措施至关重要。

结果

噻虫砜的放射性标记结合实验([(3)H] -甲基-SFX)在烟粉虱的膜上进行,证明噻虫砜与烟粉虱 nAChR 总池中的一个亚群中存在的高亲和力吡虫啉结合位点特异性相互作用。在竞争研究中,吡虫啉类似的新烟碱类杀虫剂以皮摩尔浓度置换[(3)H] -甲基-SFX。噻虫砜对暴露在原位的蚜虫神经系统的影响类似于吡虫啉和啶虫脒的影响,最后,在具有β-nAChR 中单个氨基酸点突变(R81T)的烟粉虱品系(克隆 FRC)中不存在高亲和力的噻虫砜结合位点,该区域对于新烟碱类杀虫剂的相互作用至关重要。

结论

噻虫砜在蚜虫中的烟碱型乙酰胆碱受体药理学特征与吡虫啉一致。此外,噻虫砜和目前商业化的新烟碱类杀虫剂的杀虫活性受 FRC 烟粉虱中的点突变影响。因此,建议将噻虫砜视为新烟碱类杀虫剂,并在推荐有效的杀虫剂轮作以进行抗性管理计划时考虑到这一点。

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