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黄体酮(Pro)可使KCI(60 mmol/L)或NE(1μmol/L)诱发的肌条收缩明显松驰,IC_(50)分别为70.3和93.9(μmol/L);而戊脉安(Ver)的IC_(50)则分别为0.085和0.766(μmol/L)。Pro和Ver均可使NE或CaCl_2引起的肌条收缩量效曲线右移,最大效应降低。呈非竞争性拮抗:Pro的PD_2′分别为4.072和4.688,Ver的PD_2′为5.563和6.456。无钙液中加入NE 1μmol/L引起肌条收缩(1相),再加入CaCl_22.5mmol/L引起再次收缩(2相):Pro可显著抑制上述两种收缩,而Ver仅对2相收缩有显著抑制作用。以上结果表明:黄体酮有直接扩张血管作用,它与钙拮抗剂戊脉安相似,对电压依赖性钙通道及受体调控性钙通道均有阻滞作用;此外,它还能抑制NE激活的细胞内钙的释放。
Progesterone induced a significant relaxation of muscle strips induced by KCI (60 mmol / L) or NE (1 μmol / L) with IC 50 values of 70.3 and 93.9 μmol / L, respectively. Ver) had IC50 (50) of 0.085 and 0.766 (μmol / L), respectively. Pro and Ver can make NE or CaCl2-induced contraction curve of muscle volume to the right, the maximum effect decreased. Non-competitive antagonism: Pro PD 2 ’were 4.072 and 4.688, Ver PD 2’ was 5.563 and 6.456. (1 phase) caused by the addition of NE 1 μmol / L in Ca 2+ -free fluid, and then contracted again by addition of CaCl 2 22.5 mmol / L (2 phases): Pro significantly inhibited both contractions, while Ver only contracted Significant inhibitory effect. The above results show that progesterone has a direct dilation of blood vessels, which is similar to the antagonist verapamil and has a block effect on voltage-dependent calcium channels and receptor-regulated calcium channels. In addition, it inhibits NE-activated Intracellular calcium release.