Kather H, Vogt B, Simon B
Klin Wochenschr. 1977 Jul 1;55(13):625-8. doi: 10.1007/BF01482531.
The effects of beta-adrenergic agonists such as isoproterenol, norepinephrine and epinephrine upon the adenylate cyclase activity of human fat cell ghosts were tested, each alone and in combination with the beta-blocking agent propranolol. Saturating concentrations of these agents showed a 2-6.5-fold increase of enzyme activity without addition of any artificial cofactors. Isoproterenol was more potent in stimulating the enzyme system than epinephrine and nor-epinephrine. Propranolol caused a dose-dependent rightward shift of the log-dose response curve of these beta-adrenergic agonists. The assay of human fat cell adenylate cyclase in vitro may provide a simple anc convenient assay system for the screening of beta-adrenergic drugs of potential therapeutic importance.
测试了异丙肾上腺素、去甲肾上腺素和肾上腺素等β-肾上腺素能激动剂对人脂肪细胞空壳腺苷酸环化酶活性的影响,分别单独测试以及与β-阻滞剂普萘洛尔联合测试。在不添加任何人工辅助因子的情况下,这些药物的饱和浓度使酶活性增加了2至6.5倍。异丙肾上腺素刺激酶系统的作用比肾上腺素和去甲肾上腺素更强。普萘洛尔使这些β-肾上腺素能激动剂的对数剂量反应曲线发生剂量依赖性的右移。体外测定人脂肪细胞腺苷酸环化酶可为筛选具有潜在治疗重要性的β-肾上腺素能药物提供一种简单且方便的测定系统。