Frisk-Holmberg M, Ostman J
J Pharmacol Exp Ther. 1977 Mar;200(3):598-605.
The effects of various adrenergic beta receptor agonists and antagonists on lipolysis (measured as glycerol release) in human adipose tissue in vitro were studied. Of the agonists investigated, the potency rank order was isoproteronol greater than norepinephrine greater than salbutamol. Adrenergic beta receptor blocking drugs inhibited catecholamineinduced lipolysis competitively. Propranolol was the overall most effective compound, followed by metoprolol, alprenolol and practolol, whereas butoxamine and H35/25 were weak inhibitors. The results indicate that the adrenergic reciptor mediating lipolysis in human adipose tissue is of type beta-1. Basal and theophylline-induced lipolysis was reduced when higher concentrations of these drug were used.
研究了各种肾上腺素能β受体激动剂和拮抗剂对体外人脂肪组织中脂解作用(以甘油释放量衡量)的影响。在所研究的激动剂中,效力顺序为异丙肾上腺素>去甲肾上腺素>沙丁胺醇。肾上腺素能β受体阻断药物竞争性抑制儿茶酚胺诱导的脂解作用。普萘洛尔是总体上最有效的化合物,其次是美托洛尔、阿普洛尔和普拉洛尔,而丁氧胺和H35/25是弱抑制剂。结果表明,介导人脂肪组织中脂解作用的肾上腺素能受体是β-1型。当使用更高浓度的这些药物时,基础脂解作用和茶碱诱导的脂解作用均降低。