Skoubo-Kristensen E, Fryklund J
Naunyn Schmiedebergs Arch Pharmacol. 1985 Jul;330(1):37-41. doi: 10.1007/BF00586707.
Isolated gastric glands from the rabbit were used for studying the effect of catecholamines on the release of pepsinogen. Isoprenaline, adrenaline and noradrenaline stimulated pepsinogen release in a dose-dependent manner with similar maximal effects, but isoprenaline was significantly more potent than the other two agonists. The effect was mediated through beta-adrenoceptors, since the response was inhibited by the beta-adrenoceptor antagonist, propranolol, and since the alpha-adrenoceptor agonist, phenylephrine, was without effect in the concentration range 0.01 - 10 microM. Concentration-response curves for isoprenaline were shifted to the right in parallel by increasing doses of propranolol, and maximal response was not influenced by propranolol per se, which indicates a competitive type of antagonism. A Schild plot showed a pA2-value for propranolol of 7.70 and the slope of the regression line was 1.02. Studies with the beta 1-selective antagonist pafenolol and the beta 2-selective antagonist ICI 118.551 demonstrated that isoprenaline acted through beta 1-adrenoceptors. The results suggest an adrenergic component in the control of the peptic cells in rabbit gastric mucosa.
利用兔的分离胃腺研究儿茶酚胺对胃蛋白酶原释放的影响。异丙肾上腺素、肾上腺素和去甲肾上腺素以剂量依赖方式刺激胃蛋白酶原释放，最大效应相似，但异丙肾上腺素的效力明显高于其他两种激动剂。该效应是通过β-肾上腺素能受体介导的，因为β-肾上腺素能受体拮抗剂普萘洛尔可抑制该反应，且α-肾上腺素能受体激动剂去氧肾上腺素在0.01 - 10微摩尔浓度范围内无作用。随着普萘洛尔剂量增加，异丙肾上腺素的浓度-反应曲线平行右移，且普萘洛尔本身不影响最大反应，这表明是竞争性拮抗类型。Schild图显示普萘洛尔的pA2值为7.70，回归线斜率为1.02。使用β1选择性拮抗剂阿替洛尔和β2选择性拮抗剂ICI 118.551的研究表明，异丙肾上腺素通过β1-肾上腺素能受体起作用。结果提示兔胃黏膜中胃蛋白酶细胞的控制存在肾上腺素能成分。
