克仑特罗对新生大鼠心肌细胞受磷蛋白磷酸化的作用  

Effects of Clenbuterol on Phosphorylation of Phospholamban in Neonatal Rat Cardiomyocytes

作　　者：付琴[1] 胡本容[1] 韩召敏[1] 向继洲[1] 

机构地区：[1]华中科技大学同济医学院基础医学院药理学系,武汉430030

出　　处：《华中科技大学学报（医学版）》2007年第4期441-443,共3页Acta Medicinae Universitatis Scientiae et Technologiae Huazhong

摘　　要：目的探讨β2肾上腺素受体(β2-AR)激动剂克仑特罗对培养新生大鼠心肌细胞受磷蛋白磷酸化的作用。方法测定心肌细胞搏动频率和胞内环磷酸腺苷(cAMP)水平变化的时间曲线。采用Western blot方法,检测受磷蛋白在Ser16和Thr17位点的磷酸化水平。结果克仑特罗增加新生大鼠心肌细胞搏动频率以及细胞内cAMP水平。克仑特罗还可促进受磷蛋白在Ser16位点的磷酸化,并被选择性β2-AR阻断剂ICI 118551和蛋白激酶A(PKA)抑制剂Rp-cAMP所阻断。克仑特罗还可促进受磷蛋白在Thr17位点的磷酸化。结论在新生大鼠心肌细胞β2-AR激动剂克仑特罗可促进受磷蛋白在Ser16和Thr17位点的磷酸化,并可能参与改善心脏舒张功能。Objective To investigate the effect of β2-AR agonist clenbuterol on phospholamban phosphorylation in neonatal rat cardiomyocytes. Methods The increases in beat number and intracellular cAMP were measured in cardiomyocytes exposed to clenbuterol at different incubation periods. Phosphorylation of phospholamban at serine 16 and threonine 17 was determined by Western blot using phosphospecific antibodies. Results Clenbuterol increased cardiomyocyte beats and intracellular cAMP accumulation. Phosphorylation of phospholamban at serine 16 was increased by clenbuterol and blocked by selective β2-AR antagonist ICI 118551 and PKA inhibitor Rp-cAMP. Clenbuterol increased phosphorylation of threonine 17 of phospholamban. Conclusion Activation of β2-AR promotes phosphorylation of phospholamban at serine 16 and threonine 17, thereby potentially improving diastolic function in neonatal rat cardiomyocytes.

关 键 词：克仑特罗 Β2肾上腺素受体 受磷蛋白 

分 类 号：R971[医药卫生—药品]