Pharmacological Properties of the Type 1 Tyramine Receptor in the Diamondback Moth, Plutella xylostella
Pharmacological Properties of the Type 1 Tyramine Receptor in the Diamondback Moth, Plutella xylostella
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小菜蛾 1 型酪胺受体的药理学特性
DOI：
10.3390/ijms20122953
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发表时间：
2019-06
影响因子：
5.6
通讯作者：
Zhou Xiaomao
中科院分区：
文献类型：
--
作者：
Ma Haihao;Huang Qingting;Lai Xiaoyi;Liu Jia;Zhu Hang;Zhou Yong;Deng Xile;Zhou Xiaomao
酪胺受体（TARs）可以被酪胺（TA）或章鱼胺（OA）激活，并且在一系列昆虫物种中被证明与生理调节（例如，味觉反应，社会组织和学习行为）有关。克隆了小菜蛾酪胺受体基因Pxtar1，并在HEK-293细胞系中稳定表达。分析了Pxtar1的药理特性和表达谱。酪胺可以激活PxTAR1受体，增加细胞内Ca2+浓度（(Ca2+)i）， EC50为13.1 nM，降低forskolin （10 μM）刺激的细胞内cAMP浓度（(cAMP)i）， IC50为446 nM。DPMF （amitraz的代谢物）和L(-)-香芹酮（一种精油）被发现作为PxTAR1受体激动剂。育亨宾和米安色林对PxTAR1具有明显的拮抗作用。在幼虫和成虫中，Pxtar1在头囊中表达量最高，且Pxtar1在雄性生殖器官中的表达量高于雌性生殖器官。本研究揭示了Pxtar1在小菜中的时空差异和药理特性，为筛选以Pxtar1为靶点的杀虫化合物提供了策略。
Tyramine receptors (TARs) can be activated by tyramine (TA) or octopamine (OA) and have been shown to be related to physiological regulation (e.g., gustatory responsiveness, social organization, and learning behavior) in a range of insect species. A tyramine receptor gene in Plutella xylostella, Pxtar1, was cloned and stably expressed in the HEK-293 cell line. Pharmacological properties and expression profile of Pxtar1 were also analyzed. Tyramine could activate the PxTAR1 receptor, increasing the intracellular Ca2+ concentration ((Ca2+)i) at an EC50 of 13.1 nM and reducing forskolin (10 μM)-stimulated intracellular cAMP concentration ((cAMP)i) at an IC50 of 446 nM. DPMF (a metabolite of amitraz) and L(-)-carvone (an essential oil) were found to act as PxTAR1 receptor agonists. Conversely, yohimbine and mianserin had significant antagonistic effects on PxTAR1. In both larvae and adults, Pxtar1 had the highest expression in the head capsule and expression of Pxtar1 was higher in male than in female reproductive organs. This study reveals the temporal and spatial differences and pharmacological properties of Pxtar1 in P. xylostella and provides a strategy for screening insecticidal compounds that target PxTAR1.
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影响因子：
2.7
作者：
Lange, Angela B.
通讯作者：
Lange, Angela B.
影响因子：
--
作者：
H. Torfs;W. Van Poyer;J. Poels;E. Swinnen;A. De Loof;J. Broeck
通讯作者：
H. Torfs;W. Van Poyer;J. Poels;E. Swinnen;A. De Loof;J. Broeck
影响因子：
11.4
作者：
SAUDOU, F;AMLAIKY, N;HEN, R
通讯作者：
HEN, R
DOI：
10.1007/s00359-008-0404-5
发表时间：
2009-01
期刊：
Journal of Comparative Physiology A
影响因子：
--
作者：
R. Vierk;H. Pflueger;C. Duch
通讯作者：
R. Vierk;H. Pflueger;C. Duch
影响因子：
5.6
作者：
Blenau W;Balfanz S;Baumann A
通讯作者：
Baumann A