Nasu Y
Nihon Heikatsukin Gakkai Zasshi. 1982 May;18(2):75-82.
The relaxing effect of isoprenaline on [Na+]o-free induced contracture of the guinea-pig taenia coli was investigated in presence of phentolamine (10(-5)M), an alphareceptor blocking agent. This action of isoprenaline showed dose-dependency (ED 50: 10(-5)M) and was abolished completely by beta-receptor blocking agent (propranolol, 10(-5)M). The effect of isoprenaline (10(-5)M) disappeared gradually during long exposure to [Na+]o-free solution and when short application of sodium ions to the perfusing solution, the effect of isoprenaline was restored. Pretreatment of [K+]o-free solution or ouabain (10(-5)M) enhanced the effect of isoprenaline. The effect of isoprenaline is inhibited by ouabain (10(-5)M) by about 50%. These observations strongly suggest that the inhibitory effect of isoprenaline may be mainly mediated through activation of Na-pump. However, direct activation of the drug on Na+-Ca2+ exchange, Ca-pump, or Ca-uptake into cellular Ca store sites can not be ruled out.
在存在α受体阻断剂酚妥拉明(10⁻⁵M)的情况下,研究了异丙肾上腺素对无钠诱导的豚鼠结肠带挛缩的舒张作用。异丙肾上腺素的这一作用呈剂量依赖性(半数有效剂量:10⁻⁵M),并被β受体阻断剂(普萘洛尔,10⁻⁵M)完全消除。在长时间暴露于无钠溶液期间,异丙肾上腺素(10⁻⁵M)的作用逐渐消失,而当向灌注溶液中短暂加入钠离子时,异丙肾上腺素的作用得以恢复。用无钾溶液或哇巴因(10⁻⁵M)预处理可增强异丙肾上腺素的作用。哇巴因(10⁻⁵M)可使异丙肾上腺素的作用抑制约50%。这些观察结果强烈表明,异丙肾上腺素的抑制作用可能主要通过激活钠泵介导。然而,不能排除该药物对钠钙交换、钙泵或钙摄入细胞钙储存位点的直接激活作用。