Mikkelsen E O, Poulsen S H, Christensen S B
Institute of Pharmacology, University of Aarhus, Denmark.
Pharmacol Toxicol. 1992 Feb;70(2):152-6. doi: 10.1111/j.1600-0773.1992.tb00447.x.
The effect of thapsigargin, 10(-9)-10(-6) M, and Bay K 8644, 10(-9)-10(-7) M, was studied on isolated portal veins and cardiac muscles from rats. In rat portal veins thapsigargin induced a concentration dependent increase in the amplitude of the spontaneous mechanical activity without increasing the frequency of spontaneous activity. Thapsigargin was less effective than Bay K 8644 in increasing the amplitude of the mechanical activity. In contrast to thapsigargin Bay K 8644, 10(-6) M increases the frequency of the mechanical activity. Atropine, 10(-6) M, and phentolamine, 10(-6) M, had no effect on the thapsigargin and Bay K 8644 induced increase in mechanical activity. Nitrendipine, 10(-6) M, totally abolished the mechanical response in preparations stimulated by thapsigargin and Bay K 8644. In rat atrial and papillary muscles Bay K 8644 increases the frequency in right atrium and tension in both atrial and papillary muscles. Thapsigargin was without effect on the frequency and tension in the cardial preparations. In conclusion, thapsigargin increases the amplitude of spontaneous activity in rat portal veins. In contrast to Bay K 8644 thapsigargin was less effective in increasing the amplitude and had no effect on the frequency of spontaneous activity; furthermore, thapsigargin was without effect on cardiac muscles. The results support the view that an endoplasmatic Ca2(+)-pump sensitive to thapsigargin is of importance for spontaneous activity in portal veins while such pump is of minor importance for contractile activity in cardiac muscles.
研究了毒胡萝卜素(浓度为10⁻⁹ - 10⁻⁶ M)和Bay K 8644(浓度为10⁻⁹ - 10⁻⁷ M)对大鼠离体门静脉和心肌的作用。在大鼠门静脉中,毒胡萝卜素可引起自发机械活动幅度的浓度依赖性增加,但不增加自发活动的频率。毒胡萝卜素在增加机械活动幅度方面比Bay K 8644效果差。与毒胡萝卜素相反,10⁻⁶ M的Bay K 8644可增加机械活动的频率。10⁻⁶ M的阿托品和10⁻⁶ M的酚妥拉明对毒胡萝卜素和Bay K 8644诱导的机械活动增加无影响。10⁻⁶ M的尼群地平完全消除了毒胡萝卜素和Bay K 8644刺激的标本中的机械反应。在大鼠心房和乳头肌中,Bay K 8644增加右心房的频率以及心房和乳头肌的张力。毒胡萝卜素对心脏标本的频率和张力无影响。总之,毒胡萝卜素增加大鼠门静脉自发活动的幅度。与Bay K 8644相比,毒胡萝卜素在增加幅度方面效果较差,且对自发活动频率无影响;此外,毒胡萝卜素对心肌无影响。这些结果支持以下观点:对内质网Ca²⁺泵敏感的毒胡萝卜素对门静脉的自发活动很重要,而这种泵对心肌的收缩活动不太重要。