激动剂和抑制剂影响m2毒蕈碱乙酰胆碱受体磷酸化的试验研究

The experiment study of m2 muscarinic acetylcholine receptors phosphorycation effected by agonist and inhibitor

目的 探讨受激活剂或抑制剂影响的G蛋白偶联受体激酶2（G-protein coupled receptor kinase 2,GRK2）介导的胆碱能m2受体磷酸化的调节机制.方法 本实验以纯化的大鼠脑毒蕈碱乙酰胆碱m2受体（muscarinic acetylcholine m2 receptor,mAChR2）为研究对象,观察氨甲酰胆碱、阿托品和肝素分别对m2受体磷酸化过程的影响.结果 显示氨甲酰胆碱明显增强m2受体的磷酸化,而阿托品或肝素（GRK2抑制剂）完全阻断了m2受体的磷酸化.m2受体的磷酸化是依赖激活剂作用发生的.结论 说明阿托品可以直接与m2受体结合.揭示了氨甲酰胆碱和阿托品等一些m2受体的激活剂及抑制剂对M2受体磷酸化的调节作用.

Objective The adjustment mechanism of activators or inhibitors on the G protein - coupled receptor kinase 2 （GRK2） - mediated phosphorylation of acetylcholine m2 receptor were consideration. Methods in this experiment, the muscarinic acetylcholine m2 receptor （mAChR2） of purified rat brain were studied as research subject, the effect of carbachol, atropine and heparin, respectively act on phosphorylation process to m2 receptor were observed. Result the results showed that carbachol significantly increased the phosphorylation of m2 receptors, and atropine, or heparin （GRK2 inhibitor） completely blocked the process. It means phosphorylation of m2 receptor is dependent on the activator function. Conclusion The results show that atropine directly binding with m2 receptors. Revealed carbaehol , atropine and some other activators or inhibitors were influential to the phosphorylatio of m2 receptor.