Effect of CL316,243, a highly specific beta(3)-adrenoceptor agonist, on lipolysis of epididymal, mesenteric and subcutaneous adipocytes in rats.

Effect of CL316,243, a highly specific beta(3)-adrenoceptor agonist, on lipolysis of epididymal, mesenteric and subcutaneous adipocytes in rats.
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CL316,243(一种高度特异性的β(3)-肾上腺素受体激动剂)对大鼠附睾、肠系膜和皮下脂肪细胞脂肪分解的影响。

DOI:
10.1507/endocrj.44.181
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发表时间:
1997
期刊:
影响因子:
2
通讯作者:
M. Kondo
M. Kondo
中科院分区:
医学4区
文献类型:
--
作者:
T. Umekawa;T. Yoshida;N. Sakane;M. Kondo

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为了阐明β(3)-肾上腺素受体激动剂在内脏脂肪细胞中的脂解作用是否比在皮下脂肪细胞中的脂解作用更强,在大鼠的脂肪组织中研究了由CL 316,243(一种高度特异性的β(3)-肾上腺素受体激动剂(对β(1)-、β(2)-和β(3)-受体的相对选择性分别为0、1和10,000)诱导的脂解作用。从雄性Wistar大鼠(体重约150 g)的皮下、肠系膜和附睾白色脂肪组织制备白色脂肪细胞。我们的研究结果表明,白色脂肪细胞的脂解被非特异性β-肾上腺素受体激动剂异丙肾上腺素和β 3-特异性肾上腺素受体激动剂CL 316,243刺激,但在这三种脂肪组织中,CL 316,243的脂解敏感性约为异丙肾上腺素的10倍。异丙肾上腺素和CL 316,243在附睾和肠系膜中诱导的脂解作用比在皮下脂肪细胞中的更明显,其pD 2值[EC 50的-log mol l-1(激动剂的浓度为其自身最大刺激的一半)]。这些发现表明,CL 316,243在内脏脂肪细胞中比在皮下脂肪细胞中更能脂解,尽管附睾脂肪细胞显示出与在内脏脂肪细胞中观察到的那些接近的高脂解反应。因此,CL 316,243可特别用于治疗与各种疾病相关的内脏脂肪型肥胖。
To clarify whether a beta(3)-adrenoceptor agonist is more lipolytic in the visceral adipocytes than in the subcutaneous adipocytes, the lipolysis induced by CL316,243, a highly specific beta(3)-adrenoceptor agonist (relative selectivities of 0, 1 and 10,000 for beta(1)-, beta(2)- and beta(3)-receptors, respectively) was investigated in adipose tissue from rats. White adipocytes were prepared from the subcutaneous, mesenteric, and epididymal white adipose tissues of male Wistar rats (weighing about 150 g). Our findings showed that lipolysis of white adipocytes was stimulated both by the non-specific beta-adrenoceptor agonist, isoproterenol, and by the beta(3)-specific adrenoceptor agonist, CL316,243, but the lipolytic sensitivity to CL316,243 was about 10 times greater than that to isoproterenol in these three adipose tissues. Both isoproterenol and CL316,243 induced more noticeable lipolysis in the epididymal and mesenteric than in the subcutaneous adipose cells in terms of the pD2 value [-log mol l-1 for EC50 (the concentration of an agonist giving half of its own maximum stimulation)]. These findings show that CL316,243 is more lipolytic in the visceral adipose cells than in the subcutaneous adipose cells, although epididymal adipose cells showed a high lipolytic response close to those observed in visceral adipose cells. CL316,243 may therefore be especially useful for the treatment of visceral fat type obesity related to various diseases.
大鼠不同解剖位置的白色脂肪组织中激素敏感性脂肪酶表达的差异。
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发表时间: 1982
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