Yildiz O, Ciçek S, Ay I, Tatar H, Tuncer M
Department of Pharmacology, GATA Gülhane Faculty of Medicine, Ankara, Turkey.
J Cardiovasc Pharmacol. 1996 Jul;28(1):6-10. doi: 10.1097/00005344-199607000-00002.
We wished to characterize the 5-hydroxytryptamine (5-HT) receptors mediating vasoconstriction in the human internal mammary artery (IMA). Segments of the IMA obtained from patients undergoing coronary by-pass surgery were suspended in an organ bath and exposed to 5-HT and sumatriptan (SUM), a 5-HT1-like receptor agonist, in the presence and absence of potassium chloride (KCl) and angiotensin II. 5-HT induced concentration-dependent contractions in all quiescent and pre-contracted preparations. SUM induced small contractions in 70% of quiescent IMA rings, whereas it elicited marked and concentration-dependent contractions in all of the preparations given a moderate tone by a threshold concentration of KCl and angiotensin II. The efficacy of SUM was higher in precontracted arteries. Concentration-effect curves (CEC) of 5-HT and SUM were not affected by the 5-HT3-receptor antagonist tropisetron (1 microM). The nonselective antagonist, methiothepin (30 nM), shifted the CEC of SUM to the right. 5-HT2A-receptor antagonist, ketanserin (1 microM) inhibited responses to 5-HT, whereas it affected only the responses to the smaller concentrations of SUM. When methiothepin (30 nM) was applied in the presence of ketanserin (1 microM), a further inhibition in the responses to 5-HT was observed. These results suggest that 5-HT1-like receptors mediate the contractile action of SUM and contribute to that of 5-HT in IMA.
我们希望对介导人乳内动脉(IMA)血管收缩的5-羟色胺(5-HT)受体进行表征。从接受冠状动脉搭桥手术的患者获取的IMA节段被悬挂于器官浴槽中,并在有和没有氯化钾(KCl)及血管紧张素II的情况下,分别暴露于5-HT和舒马曲坦(SUM,一种5-HT1样受体激动剂)。5-HT在所有静息和预收缩的制剂中均诱导出浓度依赖性收缩。SUM在70%的静息IMA环中诱导出小幅度收缩,而在所有通过阈浓度的KCl和血管紧张素II给予适度张力的制剂中,它引发明显的浓度依赖性收缩。SUM在预收缩动脉中的效力更高。5-HT和SUM的浓度效应曲线(CEC)不受5-HT3受体拮抗剂托烷司琼(1 microM)的影响。非选择性拮抗剂美噻吨(30 nM)使SUM的CEC右移。5-HT2A受体拮抗剂酮色林(1 microM)抑制对5-HT的反应,而它仅影响对较低浓度SUM的反应。当在酮色林(1 microM)存在的情况下应用美噻吨(30 nM)时,观察到对5-HT反应的进一步抑制。这些结果表明,5-HT1样受体介导SUM的收缩作用,并在IMA中对5-HT的收缩作用有贡献。