Rebourcet M C, Carpéné C, Lavau M
INSERM Unité 177, Paris, France.
Biochem J. 1988 Jun 15;252(3):679-82. doi: 10.1042/bj2520679.
The aim of this study was to re-assess whether alpha 2-adrenergic receptors were present in rat adipocytes, by using UK 14304, a new and very selective alpha 2-agonist. The following observations demonstrate the presence of functional alpha 2-adrenoceptors in rat adipocytes. (1) Adipocyte lipolysis was dose-dependently inhibited by UK 14304 (maximal effect 80% at 1 microM-UK 14304, 45% at 10 microM-UK 14304, under basal or theophylline-stimulated conditions respectively). (2) UK 14304 bound specifically to purified plasma membranes, with Bmax. = 744 fmol/mg of protein and KD = 9 nM. (3) The effect of UK 14304 was suppressed by alpha 2-antagonists. (4) Adrenaline inhibited lipolysis upon beta-adrenergic blockade (propranolol). (5) The anti-lipolytic effect of UK 14304 was modulated by the age of the rats.
本研究的目的是通过使用新型且极具选择性的α2-激动剂UK 14304,重新评估大鼠脂肪细胞中是否存在α2-肾上腺素能受体。以下观察结果证明大鼠脂肪细胞中存在功能性α2-肾上腺素能受体。(1)UK 14304剂量依赖性地抑制脂肪细胞脂解(在基础或茶碱刺激条件下,最大效应分别为:1 μM UK 14304时为80%,10 μM UK 14304时为45%)。(2)UK 14304与纯化的质膜特异性结合,Bmax. = 744 fmol/mg蛋白质,KD = 9 nM。(3)UK 14304的作用被α2-拮抗剂抑制。(4)肾上腺素在β-肾上腺素能阻断(普萘洛尔)后抑制脂解。(5)UK 14304的抗脂解作用受大鼠年龄的调节。