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目的探讨雌酚酮衍生物EA303对家兔离体空肠平滑肌的作用及其机制。方法以家兔离体空肠平滑肌条为标本,观察EA303对空肠平滑肌自主活动的影响;通过对比0.1μmol.L-1普萘洛尔孵育前后EA303对高钾液(KC l)和氯化乙酰胆碱的舒张量效曲线,研究EA303对β受体的作用及对氯化钙累积收缩量效曲线的影响,并与维拉帕米相比较。结果10~100μmol.L-1EA303可以剂量依赖性地降低家兔离体空肠平滑肌自发性收缩的张力和振幅;加入0.1μmol.L-1普萘洛尔孵育后,EA303对高钾液(KC l)和氯化乙酰胆碱收缩的空肠平滑肌的舒张量效曲线发生明显变化,EA303对KC l引起收缩的舒张作用被抑制,对氯化乙酰胆碱引起收缩的舒张作用被增强。1、3μmol.L-1EA303或0.1μmol.L-1维拉帕米都使CaC l2累积收缩量效曲线呈剂量依赖性右移,且最大反应降低;EA303和维拉帕米对氯化乙酰胆碱引起的第Ⅰ时相、第Ⅱ时相的收缩有明显影响。结论EA303舒张空肠平滑肌作用与β受体有关;EA303舒张作用与维拉帕米相似,可阻断电压依赖性钙通道和抑制细胞内钙释放。
Objective To investigate the effect and mechanism of estrone derivative EA303 on isolated jejunum smooth muscle of rabbits. Methods The effect of EA303 on the spontaneous activity of jejunum smooth muscle in rabbits was observed in vitro. The effects of EA303 on the activity of KC1 and acetylcholine chloride were compared before and after incubation with 0.1 μmol·L-1 propranolol Diastolic dose-response curves were used to investigate the effect of EA303 on the beta-receptor and its effect on the cumulative dose-response curve of calcium chloride, compared with that of verapamil. Results 10 ~ 100μmol.L-1EA303 could reduce the tension and amplitude of spontaneous contraction in isolated jejunum smooth muscle of rabbits in a dose-dependent manner. When EA303 was incubated with 0.1μmol.L-1 propranolol, ) And acetylcholine chloride contraction of the jejunum smooth muscle relaxation volume effect curve changes significantly, EA303 on KC l contraction caused by the inhibition of relaxation, acetylcholine contraction caused by the contraction was enhanced. 1,3μmol.L-1EA303 or 0.1μmol.L-1 verapamil all caused a dose-dependent shift in the cumulative contractile volume-effect curve of CaCl 2, and the maximal response was decreased. EA303 and verapamil induced acetylcholine Of the first phase, the second phase of contraction had a significant effect. Conclusions The relaxation of jejunal smooth muscle of EA303 is related to β receptor. The relaxation of EA303 is similar to that of verapamil, and can block the voltage-dependent calcium channel and inhibit the intracellular calcium release.