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目的：观察８个倍半萜类化合物对二氢吡啶类受体结合的作用和对离体血管张力的影响。方法：用［３Ｈ］尼群地平对猪心室肌微粒体膜受体结合方法和家兔离体血管条实验对化合物的体外作用进行研究。结果：化合物Ⅰ、Ⅱ、Ⅲ对尼群地平与受体结合有明显抑制作用，其ＩＣ５０分别为２．０×１０－５ｍｏｌ·Ｌ－１，２．７×１０－５ｍｏｌ·Ｌ－１和３．９×１０－５ｍｏｌ·Ｌ－１，其余化合物作用较弱。这些化合物抑制受体结合的作用强度与结构中母核与取代基的改变有关，而取代基的变化对活性的影响更重要。化合物Ⅱ、Ⅲ对高Ｋ＋引起的兔胸主动脉收缩有剂量依赖性的抑制作用。结论：这类化合物有钙拮抗作用，作用机制可能与影响二氢吡啶类受体有关；它们作用有量效关系和构效关系，提示有以此为先导进行深入结构改造和构效关系研究的价值。
OBJECTIVE: To observe the effect of 8 sesquiterpenoids on the binding of dihydropyridine receptors and the effect on vascular tone in vitro. METHODS: The in vitro effects of compounds were studied by [3H]-nitrendipine on pig ventricular myocyte microsomal membrane receptor binding and rabbit vascular strip experiments. RESULTS: Compounds I, II and III significantly inhibited the binding of nitrendipine to the receptors with IC50 of 2.0×10-5 mol·L-1, 2.7×10-5 mol·L-1 and 3, respectively. .9×10-5 mol·L-1, the remaining compound is weak. The inhibitory effect of these compounds on receptor binding is related to changes in the structure of the nucleus and substituents in the structure, and the effect of the substituent on the activity is more important. Compounds II and III had a dose-dependent inhibitory effect on high K+ induced contraction of rabbit thoracic aorta. Conclusion: These compounds have calcium antagonism, and their mechanism of action may be related to the effect of dihydropyridine receptors; they have a dose-effect relationship and structure-activity relationship, suggesting that this is a precursor for deep structural modification and structure-activity relationship studies. value.