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埃及伊蚊气管细胞和后肠相关神经中存在的5-HT7样受体的体外表达及药理学研究

In vitro expression and pharmacology of the 5-HT7-like receptor present in the mosquito Aedes aegypti tracheolar cells and hindgut-associated nerves.

作者信息

Lee D W, Pietrantonio P V

机构信息

Department of Entomology, Texas A & M University, College Station, TX 77843-2475, USA.

出版信息

Insect Mol Biol. 2003 Dec;12(6):561-9. doi: 10.1046/j.1365-2583.2003.00441.x.

Abstract

We have previously reported the cloning of a 5-hydroxytryptamine receptor (Aedes 5-HT7-like receptor) from adult Aedes aegypti. For functional expression of the Aedes 5-HT7-like receptor, CHO-K1 cells were stably transfected with a receptor expression construct, pC5-HT7. The Aedes 5-HT7-like receptor positively coupled to Gs protein, increasing intracellular cAMP in response to 5-HT; adenylyl cyclase activity was induced in a concentration-dependent, saturable manner. Only 5-HT, and not octopamine, dopamine or tyramine, caused the induction of cAMP. At 10 nM 5-HT a weak synergism was observed between octopamine and 5-HT. Other known agonists of the mammalian 5-HT7 receptor were tested. Their order of potency was: 5-HT >> 5-CT = 8-OH-DPAT >> pimozide. This is the first report on the functional expression of a mosquito neurohormone receptor.

摘要

我们之前报道过从成年埃及伊蚊中克隆出一种5-羟色胺受体(伊蚊5-HT7样受体)。为了实现伊蚊5-HT7样受体的功能性表达,用受体表达构建体pC5-HT7对CHO-K1细胞进行稳定转染。伊蚊5-HT7样受体与Gs蛋白呈正偶联,对5-HT作出反应时可增加细胞内cAMP;腺苷酸环化酶活性以浓度依赖性、可饱和的方式被诱导。只有5-HT,而非章鱼胺、多巴胺或酪胺,能引起cAMP的诱导。在10 nM 5-HT时,观察到章鱼胺和5-HT之间有微弱的协同作用。对哺乳动物5-HT7受体的其他已知激动剂进行了测试。它们的效力顺序为:5-HT >> 5-CT = 8-OH-DPAT >> 匹莫齐特。这是关于蚊子神经激素受体功能性表达的首次报道。

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