Modulation by neonicotinoids of honeybee α1/chicken β2 hybrid nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes,Pesticide Biochemistry and Physiology

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Modulation by neonicotinoids of honeybee α1/chicken β2 hybrid nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes
Pesticide Biochemistry and Physiology ( IF 4.2 ) Pub Date : 2020-06-01 , DOI: 10.1016/j.pestbp.2020.02.011
Sho Shigetou ₁ , Shota Shimada ₁ , Ihara Makoto ₁ , Kazuhiko Matsuda ₂

Affiliation

Neonicotinoids targeting insect nicotinic acetylcholine (ACh) receptors (insect nAChRs) are used for crop protection, but there is a concern about adverse effects on pollinators such as honeybees (Apis mellifera). Thus, we investigated the agonist actions of neonicotinoids (imidacloprid, thiacloprid and clothianidin) on A. mellifera α1 (Amα1)/chicken β2 hybrid nAChRs in Xenopus laevis oocytes according to the subunit stoichiometry of (Amα1)3(β2)2 and (Amα1)2(β2)3 using voltage-clamp electrophysiology. ACh activated (Amα1)3(β2)2 and (Amα1)2(β2)3 nAChRs with similar current amplitude. We investigated the agonist activity of imidacloprid, thiacloprid and clothianidin for the two hybrid nAChRs and found that: 1) imidacloprid showed higher affinity than clothianidin, whereas clothianidin showed higher efficacy than imidacloprid for the nAChRs; 2) Thiacloprid showed the highest agonist affinity and the lowest efficacy for the nAChRs. The Amα1/β2 subunit ratio influenced the efficacy of imidacloprid and thiacloprid, but hardly affected that of clothianidin. Hydrogen bond formation by the NH group in clothianidin with the main chain carbonyl of the loop B may account, at least in part, for the unique agonist actions of clothianidin on the hybrid nAChRs tested.

中文翻译：

新烟碱对非洲爪蟾卵母细胞中表达的蜜蜂α1/鸡β2杂合烟碱乙酰胆碱受体的调节

靶向昆虫烟碱乙酰胆碱 (ACh) 受体 (昆虫 nAChR) 的新烟碱类药物用于作物保护，但人们担心对蜜蜂 (Apis mellifera) 等传粉媒介产生不利影响。因此，我们根据 (Amα1)3(β2)2 和 (Amα1)3(β2)2 的亚基化学计量学研究了新烟碱类（吡虫啉、噻虫啉和噻虫胺）对非洲爪蟾卵母细胞中的非洲爪蟾α1（Amα1）/鸡 β2 杂合 nAChRs 的激动剂作用。 )2(β2)3 使用电压钳电生理学。ACh 激活的 (Amα1)3(β2)2 和 (Amα1)2(β2)3 nAChRs 具有相似的电流幅度。我们研究了吡虫啉、噻虫啉和噻虫胺对两种杂化 nAChR 的激动剂活性，发现：1) 吡虫啉比噻虫胺表现出更高的亲和力，而噻虫胺对 nAChR 表现出比吡虫啉更高的功效；2) 噻虫啉对 nAChRs 显示出最高的激动剂亲和力和最低的功效。Amα1/β2亚基比值影响吡虫啉和噻虫啉的药效，但几乎不影响噻虫胺的药效。噻虫胺中的 NH 基团与环 B 的主链羰基形成的氢键可能至少部分解释了噻虫胺对所测试的杂化 nAChR 的独特激动剂作用。

更新日期：2020-06-01

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