Marketing Section, Product Promotion Department, Agrochemical Division, Nippon Soda Co., Ltd., 7-2 Marunouchi 2-Chome, Chiyodaku, Tokyo 100-7010, Japan; Business Strategy and Administration Department, Chemical Business Division, Nippon Soda Co., Ltd.,.
Insecticide Group, Biological Research Department, Research and Innovation Center, Nippon Soda Co., Ltd., 345 Takada, Odawara, Kanagawa 250-0216, Japan.
Pestic Biochem Physiol. 2024 Sep;204:106074. doi: 10.1016/j.pestbp.2024.106074. Epub 2024 Aug 8.
Resistance to insecticides and acaricides is a major impediment to effectively controlling insect pests worldwide. These pests include the two-spotted spider mite Tetranychus urticae (T. urticae), which exists globally. This polyphagous herbivore causes major agricultural problems and can develop resistance to the agents above. Therefore, the continuous development of acaricides with new modes of action is important to circumvent the resistance of insects to pesticides. Acynonapyr is a novel class of acaricides containing an azabicyclo ring. In this study, we determined the activity of acynonapyr and its analogs on calcium-activated potassium (K2) channels in two-spotted spider mites using electrophysiological techniques (patch-clamp). We also examined their acaricidal efficacy against mites in the laboratory. The acynonapyr and analogs blocked T. urticae K2 (TurK2) channels in a concentration-dependent manner. A comparison of acaricidal activity against T. urticae with inhibitory activity against TurK2 revealed that TurK2 channels are the primary toxicological targets. Finally, we examined the effect of acynonapyr on Homo sapiens K2 (HsaK2.2) channels and demonstrated that the compound at 10 μM had a limited effect on the activity of this channel.
抗药性和杀螨剂是有效控制世界范围内害虫的主要障碍。这些害虫包括全球存在的二斑叶螨（Tetranychus urticae）。这种多食性的食草动物会导致严重的农业问题，并可能对上述药剂产生抗药性。因此，不断开发具有新作用模式的杀螨剂对于规避昆虫对农药的抗药性至关重要。醋炔诺孕酮是一类新型的杀螨剂，含有一个氮杂双环。在这项研究中，我们使用电生理学技术（膜片钳）测定了醋炔诺孕酮及其类似物对二斑叶螨钙激活钾（K2）通道的活性。我们还在实验室中检测了它们对螨虫的杀螨功效。醋炔诺孕酮和类似物以浓度依赖的方式阻断了二斑叶螨 K2（TurK2）通道。将杀螨活性与对 TurK2 的抑制活性进行比较表明，TurK2 通道是主要的毒理学靶标。最后，我们研究了醋炔诺孕酮对人类 K2（HsaK2.2）通道的影响，并证明该化合物在 10 μM 时对该通道的活性仅有有限的影响。
