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Neonicotinoids and Other Insect Nicotinic Receptor Competitive Modulators: Progress and Prospects
Annual Review of Entomology ( IF 15.0 ) Pub Date : 2018-01-11 00:00:00 , DOI: 10.1146/annurev-ento-020117-043042
John E. Casida 1
Affiliation  

Neonicotinoids (neonics) are remarkably effective as plant systemics to control sucking insects and for flea control on dogs and cats. The nitroimines imidacloprid, clothianidin, thiamethoxam, and dinotefuran are the leaders among the seven commercial neonics that also include the nitromethylene nitenpyram, the nitromethylene-derived cycloxaprid, and the cyanoimines acetamiprid and thiacloprid. Honey bees are highly sensitive to the nitroimines and nitromethylenes, but the cyanoimines are less toxic. All neonics are nicotinic acetylcholine receptor (nAChR) agonists with a common mode of action, target-site cross-resistance, and much higher potency on insect than mammalian nAChRs at defined binding sites. The structurally related sulfoximine sulfoxaflor and butenolide flupyradifurone are also nAChR agonists, and the mesoionic triflumezopyrim is a nAChR competitive modulator with little or no target-site cross-resistance. Some neonics induce stress tolerance in plants via salicylate-associated systems. The neonics in general are readily metabolized and, except for pollinators, have favorable toxicological profiles.

中文翻译:


新烟碱类和其他昆虫烟碱受体竞争性调节剂:进展和前景。

新烟碱类(neonics)作为植物内吸系统,对控制吮吸昆虫和对猫狗的跳蚤控制非常有效。亚硝基吡虫啉,噻虫胺,噻虫嗪和二甲呋喃是七种商业尼古丁中的佼佼者,其中还包括亚硝基硝苯并吡喃,亚硝基衍生的环磷酰胺和氰胺对乙酰氨基酚和噻虫啉。蜜蜂对亚硝基亚胺和亚硝基亚胺高度敏感,但氰胺的毒性较小。所有neonics都是烟碱型乙酰胆碱受体(nAChR)激动剂,具有共同的作用方式,靶位交叉抗性,并且在昆虫上对昆虫的效力比在定义的结合位点处的哺乳动物nAChR高得多。与结构相关的磺胺嘧啶磺胺嘧啶和丁烯内酯氟吡呋喃也是nAChR激动剂,中离子三氟甲嘧啶是一种nAChR竞争性调节剂,几乎没有目标位交叉抗性。一些神经元通过水杨酸酯相关系统诱导植物的胁迫耐受性。一般而言,新药易于代谢,除授粉剂外,还具有良好的毒理学特征。

更新日期:2018-01-11
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