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目的:比较MC9204和nifedipine(NIF)的扩血管强度,并观察MC9204是否具有血管选择性作用。方法:采用离体血管张力实验法,观察MC9204和NIF的扩血管作用。结果:MC9204和NIF对KCl、CaCl2和去甲肾上腺素(NE)引起的离体兔动脉环收缩反应均具有显著的拮抗作用,使剂量-效应曲线右移。在NE双相收缩实验中,二药均可显著抑制NE依外Ca2+性收缩反应,而对NE依内Ca2+性收缩反应无抑制作用。结论:MC9204扩血管作用强于NIF,MC9204对肾动脉和肠系膜上动脉的抑制作用强于腹主动脉,具有一定的血管选择性作用,此作用通过抑制细胞外Ca2+的进入而实现。
Objective: To compare the vasodilator intensity of MC9204 and nifedipine (NIF) and to observe whether MC9204 has vasoconstrictor effect. Methods: Vascular tension test was used to observe the vasodilatation of MC9204 and NIF. RESULTS: Both MC9204 and NIF had significant antagonistic effects on the contractile responses of isolated rabbit arterial rings induced by KCl, CaCl2 and norepinephrine (NE), shifting the dose-response curve to the right. In NE biphasic contractility test, the two drugs can significantly inhibit NE Ca2 + contractile response outside, while on NE Ca2 + contractile response was no effect. CONCLUSION: The effect of vasodilation of MC9204 is stronger than that of NIF. The inhibitory effect of MC9204 on the renal artery and superior mesenteric artery is stronger than that of the abdominal aorta. It has certain vasoconstrictor effect, which can be achieved by inhibiting the entry of extracellular Ca2 +.