过刊浏览

去甲肾上腺素引起的#alpha#_(1)肾上腺素受体三种亚型脱敏过程的差异

张幼怡, 田斌, 陈松海, 李艳芳, 韩启德

北京医科大学第三医院血管医学研究所.北京 100083

摘要

将含有#alpha#_(1)肾上腺素受体(#alpha#_(1)-AR)三种亚型的全长cDNA质粒分别转染到人胚胎肾脏细胞(HEK 293),#alpha#_(1A)-,#alpha#_(1B)-和#alpha#_(1D)-AR在HEK 293细胞株上得到高水平稳定表达(B_(max)达pmol/mg水平)用~(3)H-inositol标记和柱层析法测定细胞磷酸肌醇蓄积。观察在去甲肾上腺素(NE)长期作用下#alpha#_(1)三种受体亚型介导磷酸肌醇蓄积敏感性降低的差别。结果表明,#alpha#_(1)三种受体亚型介导的磷酸肌醇蓄积效应的减弱与NE预温育的时间和浓度呈依赖关系。在激动剂持续作用下#alpha#_(1)三种受体亚型发生脱敏的过程不同,其中#alpha#_(1A)-AR脱敏发生最快,脱敏所需NE的浓度最低;#alpha#_(1D)-AR脱敏最慢,所需NE的浓度最高;#alpha#_(1B)-AR介于上述两者之间。

关键词： α1肾上腺素受体; 激动剂; 脱敏; 受体亚型; 磷酸肌醇

Differnt susceptibilities to desensitization of three #alpha#_(1)-adrenoceptor subtypes induced by sustained norepinephrine stimulation

Zhang Youyi, Tian Bin, Chen Shonghai, Li Yanfang, Han Qide

Institute of Vascular Medicine, Third Hospital, Beijing Medical University. Beijing 100083

Abstract

cDNAs for the bovine #alpha#_(1A)-,hamster #alpha#_(1B)- and rat #alpha#_(1D)-adrenoceptors (AR) were transfected into human embryonic kidney 293 (HEK 293) cells by calcium phosphate precipitation and stably expressed at high levels. The inositol phosphates (InsPs) accumulation was measured by the method of ~(3)H-inositol incorporation and column chromatography. Susceptibilities to the desensitizaton of #alpha#_(1)-AR subtypes-mediated InsPs accumulation were determined in HEK 293 cells stimulated sustainedly by norepinephrine (NE).The NE-induced InsPs accumulation showed progressive decrease by NE pretreatment with increasing time of preincubation and concentration of NEin the cells transfected with all the #alpha#_(1)-AR subtypes. However, susceptibilities to the desensitization were different among the three subtypes. The desensitization of #alpha#_(1A)-AR took place earliest and needed lowest concentration of NE. The desensitization of #alpha#_(1D)-AR appeared to be the latest and needed hightest concentration of NE, while #alpha#_(1B)-AR stood in between.

Key words: #alpha#_1-adrenoceptor;Agonist;Desensitization;Receptor subtypes;Inositol phosphates

收稿日期：　　录用日期：

通讯作者：　　E-mail:

引用本文：

张幼怡, 田斌, 陈松海, 李艳芳, 韩启德. 去甲肾上腺素引起的#alpha#_(1)肾上腺素受体三种亚型脱敏过程的差异[J]. 生理学报 1997; 49 (1): .

Zhang Youyi, Tian Bin, Chen Shonghai, Li Yanfang, Han Qide. Differnt susceptibilities to desensitization of three #alpha#_(1)-adrenoceptor subtypes induced by sustained norepinephrine stimulation. Acta Physiol Sin 1997; 49 (1): (in Chinese with English abstract).