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沙丁胺醇和布托沙明对人脂肪细胞腺苷酸环化酶的作用。

Effects of salbutamol and butoxamine on the human fat cell adenylate cyclase.

作者信息

Kather H, Simon B

出版信息

Horm Metab Res. 1980 Dec;12(12):695-7. doi: 10.1055/s-2007-999234.

Abstract

In order to characterize the beta-adrenoceptors coupled to the human fat cell adenylate cyclase more extensively the effects of the beta 2-selective agonist salbutamol on basal and isoproterenol-stimulated rates of cAMP-accumulation were studied. Although exhibiting only low intrinsic activity salbutamol displayed only slightly lower affinity towards the beta-adrenoceptors linked to the human fat cell adenylate cyclase than isoproterenol. In addition, the beta 2-selective antagonist butoxamine was slightly more potent in inhibiting the isoproterenol-stimulated fat cell enzyme than the cardioselective beta-blocking agent practolol. These results further emphasize the difficulties in classifying the lipolytic response of adipose tissue to beta-adrenergic agonists and antagonists within a uniform beta-receptor theory.

摘要

为了更全面地表征与人类脂肪细胞腺苷酸环化酶偶联的β-肾上腺素能受体,研究了β2选择性激动剂沙丁胺醇对基础和异丙肾上腺素刺激的环磷酸腺苷(cAMP)积累速率的影响。尽管沙丁胺醇仅表现出较低的内在活性,但其对与人类脂肪细胞腺苷酸环化酶相连的β-肾上腺素能受体的亲和力仅略低于异丙肾上腺素。此外,β2选择性拮抗剂布托沙明在抑制异丙肾上腺素刺激的脂肪细胞酶方面比心脏选择性β阻滞剂普拉洛尔略强。这些结果进一步强调了在统一的β受体理论内对脂肪组织对β-肾上腺素能激动剂和拮抗剂的脂解反应进行分类的困难。

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