血管内皮细胞上嘌呤受体新亚型对血管张力的调节作用

Pharmacological Characteristics of Novel Endothelium Purinoceptor in Modulating Vascular Tone

目的研究血管内皮细胞上嘌呤受体新亚型对血管张力调节的作用特点。方法大鼠离体主动脉环实验。结果与结论在NO释放的前提下激活血管内皮细胞上嘌呤受体新亚型可介导血管收缩反应,该受体可同时被P1受体激动剂腺苷、CPA、CPCA和P2受体激动剂ATP、ADP、UTP、2-MeSATP所激活;该受体与PTX敏感型G蛋白偶联;产生的缩血管效应与花生四烯酸的代谢密切相关,由前列腺素类缩血管物质介导,引起细胞内钙储库的释放,胞内钙升高,诱发血管收缩。

Aim To investigate the effects of novel endothelium purinoceptor on isolated rat aorta and the partial pharmacological characteristics. Methods Tones of isolated rat aorta preparations were determined using isometric force recording. Results and Conclusion The endothelium-dependent vascular contraction induced by the novel purinoceptor subtypes was dependent on the presence of nitric oxide released from endothelium. The pharmacological characteristics of the receptor could be summarized as follows ; 1 ） it can be activated by the P1 receptor agonist adenosine, CPA, CPCA and the P2 receptor agonists ATP, ADP, UTP, 2-MeSATP; 2） it is coupled to PTX-sensitive G protein; 3 ） it stimulates prostaglandin synthesis and arachidonic acid turnover and results in intracellular calcium mobilization and vascular contraction.