Oxazosulfyl, a Novel Sulfyl Insecticide, Binds to and Stabilizes the Voltage-Gated Sodium Channels in the Slow-Inactivated State,Journal of Agricultural and Food Chemistry

当前位置： X-MOL 学术 › J. Agric. Food Chem. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Oxazosulfyl, a Novel Sulfyl Insecticide, Binds to and Stabilizes the Voltage-Gated Sodium Channels in the Slow-Inactivated State
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2021-04-01 , DOI: 10.1021/acs.jafc.0c04617
Tatsuya Suzuki ₁ , Seiji Yamato ₁

Affiliation

Oxazosulfyl is the first representative of a novel sulfyl class of insecticides with a potent and cross-spectrum insecticidal activity, albeit with an unclear mechanism of action. As a potential agent of pest control in rice fields, we investigated the action of oxazosulfyl on the nervous system and voltage-gated sodium channels in insects. After the injection of 10 μg of oxazosulfyl, American cockroaches (Periplaneta americana) were quickly paralyzed, which persisted for more than 7 days. Extracellular recordings revealed a depressed spontaneous nerve activity in the cockroaches injected with oxazosulfyl, which specifically affected the voltage-gated sodium channels (in German cockroaches (Blattella germanica) expressed in Xenopus oocytes) in the slow-inactivated state resulting in the inhibition of sodium currents. The potency of oxazosulfyl and other sodium channel blockers to block sodium channels was consistent with their insecticidal activity. Thus, we conclude that the action mode of oxazosulfyl involves the state-dependent blockage of voltage-gated sodium channels.

中文翻译：

恶唑磺酰，一种新型的磺酰杀虫剂，可在慢速灭活状态下结合并稳定电压门控钠通道

恶唑磺酰基是新型磺酰基类杀虫剂的第一个代表，尽管其作用机理尚不清楚，但该类杀虫剂具有强效和跨谱杀虫活性。作为稻田害虫防治的潜在剂，我们研究了恶唑硫基对昆虫神经系统和电压门控钠通道的作用。注射10μg的恶唑硫基后，美洲蟑螂（Periplaneta americana）迅速瘫痪，持续了7天以上。细胞外记录显示，在注射恶唑磺酰的蟑螂中自发神经活动受到抑制，这特别影响了非洲爪蟾中表达的电压门控钠通道（在德国蟑螂（德国小Bl）中）卵细胞处于缓慢灭活状态，导致钠电流受到抑制。恶唑硫基和其他钠通道阻滞剂阻断钠通道的效力与其杀虫活性一致。因此，我们得出结论，恶唑硫基的作用方式涉及电压门控钠通道的状态依赖性阻断。

更新日期：2021-04-14

点击分享查看原文

点击收藏

公开下载

阅读更多本刊新发论文本刊介绍/投稿指南