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人脂肪细胞膜空泡的儿茶酚胺敏感性腺苷酸环化酶:使用不同β-肾上腺素能药物的比较研究

Catecholamine-sensitive adenylate cyclase of human fat cell ghosts: a comparative study using different beta-adrenergic agents.

作者信息

Kather H, Simon B

出版信息

Metabolism. 1977 Nov;26(11):1179-84. doi: 10.1016/0026-0495(77)90109-3.

Abstract

Some of the effects of beta-adrenergic agonists and antagonists on the adenylate cyclase system of human fat cell ghosts were studied. Isoproterenol, by causing about a fourfold increase of enzyme activity, was more potent than epinephrine and norepinephrine (about 2.5--3.0-fold stimulation). The beta2-adrenergic agonists salbutamol, terbutalin, and fenoterol were considerably less effective than the naturally occurring catecholamines. The stimulatory actions of isoproterenol and beta2-adrenergic agonists were competitively inhibited by the beta-blocking agent propranolol. Isoproterenol stimulation was also inhibited by the selective beta1-adrenergic antagonist practolol. This compound, however, was less potent than propranolol. The results are suggestive for an adenylate cyclase system in human fat cell ghosts coupled to beta1-adrenergic receptor sites. These receptors differ from the cardiac beta receptors with respect to practolol affinity.

摘要

研究了β-肾上腺素能激动剂和拮抗剂对人脂肪细胞空壳腺苷酸环化酶系统的一些作用。异丙肾上腺素使酶活性增加约四倍,比肾上腺素和去甲肾上腺素更有效(约2.5 - 3.0倍刺激)。β2-肾上腺素能激动剂沙丁胺醇、特布他林和非诺特罗的效果明显低于天然存在的儿茶酚胺。β-阻滞剂普萘洛尔竞争性抑制异丙肾上腺素和β2-肾上腺素能激动剂的刺激作用。选择性β1-肾上腺素能拮抗剂普拉洛尔也抑制异丙肾上腺素的刺激作用。然而,该化合物的效力低于普萘洛尔。结果提示人脂肪细胞空壳中的腺苷酸环化酶系统与β1-肾上腺素能受体位点偶联。就普拉洛尔亲和力而言,这些受体与心脏β受体不同。

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