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目的：探讨咖啡酸、阿魏酸和ＣＡ－ １２０１ 对ＥＴ－ １ 生物效应的拮抗作用。方法：用不同剂量的咖啡酸、阿魏酸和ＣＡ－ １２０１ 拮抗ＥＴ－ １ 引起小鼠急性死亡、缩血管效应、升压效应及致平滑肌细胞增殖效应。结果：（１） 咖啡酸、阿魏酸和ＣＡ－ １２０１ 在０－１ ～１００ ｍｇｋｇ 剂量范围内，对ＥＴ－ １ 致小鼠死亡有明显的对抗作用，该作用存在剂量依赖性；（２） 三种药物对ＥＴ－ １ 缩血管效应有明显的拮抗作用，咖啡酸和ＣＡ－ １２０１ 拮抗效能相近，而阿魏酸的拮抗效能强于咖啡酸和ＣＡ－ １２０１ ；（３） 三种药物均能拮抗ＥＴ－ １ 的升血压作用，与对照组相比，该作用有显著差异；（４） 三种药物对ＥＴ－１ 致家兔血管平滑肌细胞增殖有明显的抑制作用，该作用具剂量依赖性。结论：咖啡酸、阿魏酸和ＣＡ－ １２０１ 能有效地拮抗ＥＴ－ １ 的生物效应，是一类新的ＥＴ 拮抗剂
Objective: To investigate the antagonistic effects of caffeic acid, ferulic acid and CA-1201 on the biological effects of ET-1. Methods: Antagonism of ET-1 by different doses of caffeic acid, ferulic acid and CA-1201 induced acute death, vasoconstriction, vasopressor effect and proliferation of smooth muscle cells. Results: (1) Caffeic acid, ferulic acid and CA-1201 showed a significant antagonistic effect on the death of ET-1-induced mice in a dose range of 0-1-100 mg kg, and the effect was dose-dependent. ( 2) The three drugs obviously antagonized ET-1 vasoconstrictive effect. The antagonistic potencies of caffeic acid and CA-1201 were similar, while the antagonistic potency of ferulic acid was stronger than that of caffeic acid and CA-1201. (3) The three drugs (4) The three drugs significantly inhibited the proliferation of vascular smooth muscle cells induced by ET-1 in rabbits, and the effect was dose-dependent Dependency. CONCLUSION: Caffeic acid, ferulic acid and CA-1201 can effectively antagonize the biological effects of ET-1 and are a new class of ET antagonists