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绿盲蝽β-肾上腺素能样章鱼胺受体的分子和药理学特性研究。

Molecular and pharmacological characterization of a β-adrenergic-like octopamine receptor from the green rice leafhopper Nephotettix cincticeps.

机构信息

State Key Laboratory of Rice Biology & Ministry of Agricultural and Rural Affairs, Key Laboratory of Molecular Biology of Crop Pathogens and Insects, Institute of Insect Sciences, Zhejiang University, Hangzhou, 310058, China; College of Horticulture and Plant Protection, Yangzhou University, Yangzhou, 225009, China.

State Key Laboratory of Rice Biology & Ministry of Agricultural and Rural Affairs, Key Laboratory of Molecular Biology of Crop Pathogens and Insects, Institute of Insect Sciences, Zhejiang University, Hangzhou, 310058, China.

出版信息

Insect Biochem Mol Biol. 2020 May;120:103337. doi: 10.1016/j.ibmb.2020.103337. Epub 2020 Feb 25.

DOI:10.1016/j.ibmb.2020.103337
PMID:32109588
Abstract

As the counterparts of noradrenaline and adrenaline in vertebrates, octopamine (OA) regulates multiple physiological and behavioral processes in invertebrate. OA mediates its effects via binding to specific octopamine receptors (OARs). Functional and pharmacological characterization of OARs have been reported in several insects. However, little work was documented in hemipteran insects. We cloned a β-adrenergic-like OAR (NcOA2B2) from Nephotettix cincticeps. NcOA2B2 shares high similarity with members of the OA2B2 receptor class. Transcript level of NcOA2B2 varied in various tissues and was highly expressed in the leg. After heterologous expression in CHO-K1 cells, NcOA2B2 was dose-dependently activated by OA (EC = 2.56 nM) and tyramine (TA) (EC = 149 nM). Besides putative octopaminergic agonists, dopaminergic agonists and amitraz and DPMF potently activated NcOA2B2 in a dose-dependent manner. Receptor activity was blocked by potential antagonists and was most efficiently antagonized by asenapine. Phentolamine showed both antagonist and agonist effects on NcOA2B2. Our results offer the important information about molecular and pharmacological characterization of an OAR from N. cincticeps that will provide the basis for forthcoming studies on its roles in physiological processes and behaviors, and facilitate the design of novel insecticides for pest control.

摘要

章鱼胺(OA)作为脊椎动物去甲肾上腺素和肾上腺素的对应物,调节无脊椎动物的多种生理和行为过程。OA 通过与特定的章鱼胺受体(OAR)结合来发挥其作用。已经在几种昆虫中报道了 OAR 的功能和药理学特征。然而,在半翅目昆虫中,相关工作很少。我们从 Nephotettix cincticeps 克隆了一个β-肾上腺素样 OAR(NcOA2B2)。NcOA2B2 与 OA2B2 受体类别的成员具有高度相似性。NcOA2B2 的转录水平在各种组织中存在差异,在腿部表达水平较高。在 CHO-K1 细胞中异源表达后,NcOA2B2 被 OA(EC = 2.56 nM)和酪胺(TA)(EC = 149 nM)剂量依赖性激活。除了推定的章鱼胺激动剂外,多巴胺激动剂和阿米曲嗪和 DPMF 也以剂量依赖性方式强烈激活 NcOA2B2。受体活性被潜在的拮抗剂阻断,被asenapine 最有效地拮抗。苯肾上腺素对 NcOA2B2 既有拮抗剂作用又有激动剂作用。我们的研究结果提供了关于 N. cincticeps OAR 的分子和药理学特征的重要信息,为其在生理过程和行为中的作用的后续研究提供了基础,并为害虫防治的新型杀虫剂的设计提供了便利。

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