利多卡因对离体兔胸主动脉环收缩的影响
EFFECTS OF LIDOCAINE ON CONTRACTION OF ISOLATED RABBIT AORTIC RINGS
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摘要: 以维拉帕米(verapamil,Ver)作对照,在离体兔胸主动脉环上对利多卡因(lidocaine,Lid)松弛血管平滑肌的机理进行了探讨。Lid对高K+去极化主动脉环收缩和Ver一样有明显的松弛作用。对去甲肾上腺素(NA)引起主动脉环收缩的试验中,Lid和Ver都能抑制细胞内Ca2+的释放,但不抑制外Ca2+内流。Lid对KCl,NA量-效曲线产生非平行右移,最大反应压低,且对KCl的抑制作用大于NA,说明Lid对PDC通道有选择性阻滞作用,而对ROC通道相对不敏感。对CaCl2量-效曲线也产生非平行右移且最大反应压低,呈非竞争性拮抗。初步提示Lid在一定浓度下有拮抗Ca2+的作用,这种作用为非特异性,是松弛血管平滑肌机理之一。Abstract: The mechanism of relaxing effects of lidocaie(Lid)on the contraction of isolatedrabbit thoracic aortic rings was studied. Verapamil(Ver)was used for comparison. Lid and Vershowed obvious relaxing effect on contraction evoked by high K+ depolarization,In the study ofcontractions induced by noradrenaline(NA) ,both Lid and Ver were shown to suppress the componentelicited by calcium release from the intra-cellular store, but not that induced by calcium influx. Lidshifted the dose-response curves for KCl and NA to the right nonparallelly and depressed their maximalresponses. The inhibition to KCl was more potent than that to NA. This suggests that Lid has selectiveblocking effects on PDC channel , but not the ROC channel. Lid shifted the dose-response curve forCaCl2 to the right nonparallelly and depressed its maximal response. The results indicate that thecalcium antagonistic property of Lid may be one of the mechanisms of its vascular smooth musclerelaxing effect.
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