Agrochemicals Research Center, Mitsui Chemicals Agro, Inc., Mobara, Chiba 297-0017, Japan.
Development Department, Mitsui Chemicals Agro, Inc., Chuo-ku, Tokyo 103-0027, Japan.
Pestic Biochem Physiol. 2020 May;165:104554. doi: 10.1016/j.pestbp.2020.104554. Epub 2020 Mar 4.
Dinotefuran (DTF) is a systemic neonicotinoid insecticide characterized by a tetrahydrofuran ring. In the present study, we examined the characteristics of DTF binding to native nicotinic acetylcholine receptors (nAChRs) expressed in the American cockroach Periplaneta americana using radioligand-binding methods. The Scatchard analysis, using [H]imidacloprid (IMI), indicated that IMI has a single class of high-affinity binding sites in the P. americana nerve cord. In contrast, the Scatchard analysis using [H]DTF indicated that DTF has two different classes of binding sites. Both DTF and IMI were found to bind to one of the classes, for which DTF showed low affinity. The other class, for which DTF showed high affinity, was localized in the abdominal nerve cord but not in the thoracic nerve cord. IMI showed low affinity for the high-affinity DTF binding sites. Our data suggest that DTF binds with high affinity to a nAChR subtype distinct from the high-affinity subtype for IMI. This difference might be responsible, at least in part, for the difference in resistance development to DTF and IMI in P. americana.
二氢茉莉酮酸甲酯(DTF)是一种具有四氢呋喃环的系统新烟碱类杀虫剂。在本研究中,我们使用放射性配体结合方法研究了 DTF 与美洲大蠊 Periplaneta americana 中表达的天然烟碱型乙酰胆碱受体(nAChRs)结合的特性。使用 [H]吡虫啉(IMI)进行 Scatchard 分析表明,IMI 在美洲大蠊神经索中有一个单一的高亲和力结合位点。相比之下,使用 [H]DTF 进行 Scatchard 分析表明,DTF 具有两种不同类型的结合位点。DTF 和 IMI 都被发现与其中一种结合位点结合,而 DTF 对该结合位点的亲和力较低。DTF 显示高亲和力的另一个结合位点位于腹部神经索中,但不在胸部神经索中。IMI 对高亲和力 DTF 结合位点的亲和力较低。我们的数据表明,DTF 与不同于 IMI 的高亲和力 nAChR 亚型具有高亲和力。这种差异至少部分解释了 P. americana 对 DTF 和 IMI 产生抗性的差异。