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目的:子宫平滑肌内存在多种5-HT受体,5-HT通过作用于5-HT受体实现其对子宫收缩活性的影响。本研究探讨巴西苏木红素对5-HT受体的作用及其特点。方法:小鼠分离子宫平滑肌条,采用受体拮抗实验和real time PCR方法,对巴西苏木红素的5-HT受体的抑制作用进行研究。结果:巴西苏木红素虽然对正常子宫平滑肌的收缩幅度和频率无影响,但能明显抑制5-HT2受体激动剂马来酸麦角新碱的收缩活性,其pA2为5.71±0.21。而5-HT亚型的选择性激动剂舒马普坦(5-HT1D)、AL34662(5-HT2A)、MCPP(5-HT2C)的收缩子宫活性同样能够被巴西苏木红素抑制,pA2分别为4.58±0.06;4.91±0.15;5.38±0.15。巴西苏木红素明显抑制了5-HT受体1D和2C亚型mRNA的表达。结论:巴西苏木红素能够阻滞小鼠子宫5-HT受体,并通过可能影响5-HT受体所介导的子宫功能。
Objective: There are multiple 5-HT receptors in uterine smooth muscle. 5-HT acts on the uterine contractile activity by acting on 5-HT receptors. This study was to investigate the effect and its characteristics of 5-HT receptors in Brazil. METHODS: Mouse uterine smooth muscle strips were isolated, and the inhibitory effect of 5-HT receptors on the Brazilian hematocyanin was studied using receptor antagonistic and real time PCR methods. RESULTS: Although Brazilian hematocrit did not affect the contraction amplitude and frequency of normal uterine smooth muscle, it significantly inhibited the contractile activity of the 5-HT2 receptor agonist ergometrine maleate, with a pA2 of 5.71±0.21. The contractile uterine activity of 5-HT1D, AL34662 (5-HT2A), and MCPP (5-HT2C), selective agonists of the 5-HT subtype, was similarly suppressed by Brazilian hematocyanin, with a pA2 of 4.58. ± 0.06; 4.91 ± 0.15; 5.38 ± 0.15. Brazilian hematoxilin significantly inhibited the expression of 5-HT receptor 1D and 2C isoform mRNAs. Conclusion: Brazilian hematocyanin can block the 5-HT receptor in the mouse uterus and may affect uterine function mediated by the 5-HT receptor.