Bloomquist J R
Department of Entomology, Virginia Polytechnic Institute and State University, Blacksburg 24061-0319, USA.
Annu Rev Entomol. 1996;41:163-90. doi: 10.1146/annurev.en.41.010196.001115.
Ion channels are the primary target sites for several classes of natural and synthetic insecticidal compounds. The voltage-sensitive sodium channel is the major target site for DDT and pyrethroids, the veratrum alkaloids, and N-alkylamides. Recently, neurotoxic proteins from arthropod venoms, some of which specifically attack insect sodium channels, have been engineered into baculoviruses to act as biopesticides. The synthetic pyrazolines also primarily affect the sodium channel, although some members of this group target neuronal calcium channels as well. The ryanoids have also found use as insecticides, and these materials induce muscle contracture by irreversible activation of the calcium-release channel of the sarcoplasmic reticulum. The arylheterocycles (e.g. endosulfan and fipronil) are potent convulsants and insecticides that block the GABA-gated chloride channel. In contrast, the avermectins activate both ligand- and voltage-gated chloride channels, which leads to paralysis. At field-use rates, a neurotoxic effect of the ecdysteroid agonist RH-5849 is observed that involves blockage of both muscle and neuronal potassium channels. The future use of ion channels as targets for chemical and genetically engineered insecticides is also discussed.
离子通道是几类天然和合成杀虫化合物的主要作用靶点。电压敏感钠通道是滴滴涕、拟除虫菊酯、藜芦生物碱和N - 烷基酰胺的主要作用靶点。最近，节肢动物毒液中的神经毒性蛋白，其中一些专门攻击昆虫钠通道，已被改造成杆状病毒用作生物杀虫剂。合成吡唑啉也主要影响钠通道，尽管该类中的一些成员也靶向神经元钙通道。鱼尼丁也被用作杀虫剂，这些物质通过不可逆地激活肌浆网钙释放通道诱导肌肉挛缩。芳基杂环化合物（如硫丹和氟虫腈）是强效惊厥剂和杀虫剂，可阻断GABA门控氯离子通道。相比之下，阿维菌素激活配体门控和电压门控氯离子通道，导致麻痹。在田间使用剂量下，观察到蜕皮甾类激动剂RH - 5849的神经毒性作用，涉及肌肉和神经元钾通道的阻断。还讨论了离子通道作为化学和基因工程杀虫剂靶点的未来应用。
