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作用于烟碱型乙酰胆碱受体的杀虫剂的无脊椎动物药理学

The invertebrate pharmacology of insecticides acting at nicotinic acetylcholine receptors.

作者信息

Crossthwaite Andrew J, Bigot Aurelien, Camblin Philippe, Goodchild Jim, Lind Robert J, Slater Russell, Maienfisch Peter

机构信息

Syngenta Crop Protection, Jealott's Hill International Research Centre, Bracknell, Berkshire, RG42 6EY, UK.

Syngenta Crop Protection AG, Schaffhauserstrasse 101, CH-4332 Stein, Switzerland.

出版信息

J Pestic Sci. 2017 Aug 20;42(3):67-83. doi: 10.1584/jpestics.D17-019.

Abstract

The nicotinic acetylcholine receptor (nAChR) is a ligand-gated ion channel composed of 5 protein subunits arranged around a central cation selective pore. Several classes of natural and synthetic insecticides mediate their effect through interacting at nAChRs. This review examines the basic pharmacology of the neonicotinoids and related chemistry, with an emphasis on sap-feeding insects from the order Hemiptera, the principle pest target for such insecticides. Although the receptor subunit stoichiometry for endogenous invertebrate nAChRs is unknown, there is clear evidence for the existence of distinct neonicotinoid binding sites in native insect preparations, which reflects the predicted wide repertoire of nAChRs and differing pharmacology within this insecticide class. The spinosyns are principally used to control chewing pests such as Lepidoptera, whilst nereistoxin analogues are used on pests of rice and vegetables through contact and systemic action, the pharmacology of both these insecticides is unique and different to that of the neonicotinoids.

摘要

烟碱型乙酰胆碱受体(nAChR)是一种配体门控离子通道,由围绕中央阳离子选择性孔排列的5个蛋白质亚基组成。几类天然和合成杀虫剂通过与nAChRs相互作用来介导其作用。本综述研究了新烟碱类杀虫剂的基本药理学及其相关化学,重点关注半翅目吸食汁液的昆虫,这类昆虫是此类杀虫剂的主要害虫目标。尽管内源性无脊椎动物nAChRs的受体亚基化学计量未知,但有明确证据表明在天然昆虫制剂中存在不同的新烟碱类结合位点,这反映了预测的nAChRs种类繁多以及该类杀虫剂内不同的药理学特性。多杀菌素主要用于防治鳞翅目等咀嚼式害虫,而沙蚕毒素类似物则通过接触和内吸作用用于防治水稻和蔬菜害虫,这两种杀虫剂的药理学特性独特,与新烟碱类不同。

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