论文部分内容阅读
本文用放射配体结合实验研究了α1-肾上腺素受体(α1-AR)及亚型在大鼠左心房的分布。结果表明,大鼠左心房α1-AR有α1A与α1B两种亚型,α1A亚型约占1/3,α1B亚型占2/3。离体灌流左心房功能实验结果表明,α1-AR不同亚型对β肾上腺素受体(β-AR)所介导的正性变力反应具有不同性质的协同作用。当酚妥拉明10μmol/L同时阻断α1A与α1B亚型时,NE(同时激动α1-与β-AR)的剂量-收缩效应曲线显著左移,当用CEC20μmol/L预处理以阻断α1B亚型时,NE的剂量-收缩效应曲线则显著右移,而用WB41011nmol/L阻断α1A亚型后,NE的剂量-收缩效应曲线出现左移;此外,当用苯肾上腺素激动α1-AR时,异丙肾上腺素的剂量-收缩效应曲线亦显著右移。提示α1A亚型可抑制β-AR介导的正性变力效应,而α1B亚型则可增强β-AR所介导的反应,但当α1-AR的上述两种亚型同时激动时,则以α1A亚型的调节作用为主。
Radioligand binding experiments were used to investigate the distribution of α1-adrenoceptors (α1-AR) and its subtypes in the left atrium of rats. The results showed that α1A and α1B subtypes were present in the left atrium of the rat, accounting for about 1/3 of the α1A subtype and 2/3 of the α1B subtype. The experimental results of left atrial function in vitro perfusion showed that different subtypes of α1-AR have different synergistic effects on the positive force reaction mediated by β-adrenergic receptor (β-AR). When phentolamine 10 μmol / L blocked both α1A and α1B subtypes, the dose-contraction effect curve of NE (simultaneous agonistic α1- and β-AR) shifted significantly to the left. When pretreated with CEC 20 μmol / L to block α1B The dose-contraction effect curve of NE was significantly shifted to the right subtype, while the dose-contraction effect curve of NE appeared to shift to the left when WB41011nmol / L was used to block α1A subtype. In addition, when phenylephrine was used to agonize α1-AR , The isoproterenol dose-contraction effect curve also shifted significantly to the right. The results suggest that α1A subtype inhibits the β-AR-mediated positive force effect, whereas α1B subtype enhances β-AR-mediated responses. However, when the two subtypes of α1-AR are agonized simultaneously, Α1A subtype regulation mainly.