EFFECTS OF SELECTIVE AND NON-SELECTIVE BETA-ADRENERGIC AGENTS ON INSULIN-SECRETION INVIVO
EFFECTS OF SELECTIVE AND NON-SELECTIVE BETA-ADRENERGIC AGENTS ON INSULIN-SECRETION INVIVO
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DOI：
10.1016/0014-2999(81)90390-3
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发表时间：
1981-01-01
影响因子：
5
通讯作者：
LUNDQUIST, I
中科院分区：
文献类型：
--
作者：
AHREN, B;LUNDQUIST, I
在小鼠体内研究了不同的β-肾上腺素能药物对胰岛素分泌的影响。非选择性β刺激剂异丙基去甲肾上腺素和选择性β2刺激剂特布他林均显著刺激胰岛素分泌，具有相同的疗效，且呈剂量依赖关系。2β-激动剂后的血浆胰岛素峰值时间(5-6分钟)比葡萄糖或氨基甲胆碱刺激后的时间(1.5-2.5分钟)晚。在非常高的剂量水平下，β-刺激剂异丙氨基噻唑氧基丙醇略微增加了血浆胰岛素浓度。非选择性β受体阻滞剂心得安和β2受体阻滞剂ICI118,551[DL-erythro-l-(7-methylindan-4-yloxy)-3-isopropylamino-butan-2-ol]显著抑制特布他林诱导的胰岛素释放，但选择性β1受体阻滞剂美托洛尔仅在高剂量水平起作用。在较高剂量水平，3种阻滞剂适度抑制胰岛素对葡萄糖的反应，这表明葡萄糖的作用部分依赖完整的β-肾上腺素能受体。β2受体阻滞剂丁毒胺和β1受体阻滞剂帕马托洛尔不影响胰岛素的分泌。β-肾上腺素能受体刺激促进体内胰岛素分泌，但调节胰岛素分泌的β-肾上腺素能受体不能很好地适应β1和β2的常规细分，尽管它们显然主要是β2-型。
The effects of various .beta.-adrenergic agents on insulin secretion were investigated in vivo in mice. The non-selective .beta.-stimulator isopropylnoradrenaline and the selective .beta.2-stimulator terbutaline both stimulated insulin secretion markedly, with the same efficacy and in a dose-dependent manner. The peak levels of plasma insulin after the 2 .beta.-agonists were achieved at a later time (5-6 min) than after stimulation with glucose or carbachol (1.5-2.5 min). At very high dose levels the .beta.-stimulator isopropylaminothiazoloxypropanol slightly increased plasma insulin concentrations. The non-selective .beta.-blocker propranolol and the .beta.2-selective blocker ICI 118,551 [DL-erythro-l-(7-methylindan-4-yloxy)-3-isopropylamino-butan-2-ol] inhibited terbutaline-induced insulin release markedly and at comparable low dose levels, but the selective .beta.1-blocker metoprolol exerted this effect only at a high dose level. At higher dose levels the 3 blockers moderately depressed the insulin response to glucose suggesting a partial dependence on intact .beta.-adrenoceptors for the effect of glucose. The .beta.2-blocker butoxamine and the .beta.1-blocker pamatolol did not influence insulin secretion. .beta.-Adrenoceptor stimulation enhanced insulin secretion in vivo, but the .beta.-adrenoceptors regulating insulin secretion do not fit well into the conventional subdivision of .beta.1 and .beta.2, although they apparently are mainly of the .beta.2-type.