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目的观察吉非罗齐拮抗Bay K 8644对离体大鼠主动脉的收缩效果,并进一步研究其机制。方法采用离体血管张力记录法记录大鼠主动脉血管环的张力变化,膜片钳电生理学记录大鼠主动脉平滑肌细胞L-型电压依赖性钙电流。结果Bay K 8644可以引起大鼠主动脉血管环收缩,最大收缩幅度为(2.13±0.42)g,提前孵育吉非罗齐可以对Bay K 8644的收缩幅度起到一定程度的抑制作用,使其收缩幅度降至(1.02±0.36)g。提前孵育L-NAME和去内皮均没有对吉非罗齐的抑制效果产生明显影响。Bay K 8644可以使得大鼠主动脉平滑肌细胞L-型钙电流增大127.62%,而吉非罗齐的干预,可以使其增幅降低到79.48%。结论吉非罗齐可以一定程度上抑制Bay K 8644引起的大鼠主动脉收缩,其效果不受一氧化氮合酶抑制剂L-NAME及去内皮的影响。吉非罗齐可以部分拮抗Bay K 8644引起的大鼠离体主动脉平滑肌细胞L-型电压依赖性钙电流的增大。
Objective To observe the contractile effect of gemfibrozil antagonism Bay K 8644 on isolated rat aorta and further investigate its mechanism. Methods Tension changes of aortic rings were recorded by using in vitro vascular tone recording method. L-type voltage-dependent calcium currents were recorded by patch clamp electrophysiology in rat aortic smooth muscle cells. Results Bay K 8644 could induce contraction of aortic rings of rats with a maximum contraction amplitude of (2.13 ± 0.42) g. Premature incubation of gemfibrozil inhibited the contraction of Bay K 8644 to a certain extent and caused a contraction The amplitude dropped to (1.02 ± 0.36) g. Preincubation of L-NAME and endothelium did not have a significant effect on the inhibitory effect of gemfibrozil. Bay K 8644 could increase the L-type calcium current in rat aortic smooth muscle cells by 127.62%, while the gemfibrozil intervention could reduce the increase to 79.48%. Conclusion Gemfibrozil can inhibit the contraction of rat aorta induced by Bay K 8644 to a certain extent. The effect of gemfibrozil is not affected by L-NAME and endotheliocyte of nitric oxide synthase inhibitor. Gemfibrozil could partially antagonize the increase of L-type voltage-dependent calcium current in isolated rat aortic smooth muscle cells induced by Bay K 8644.