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血浆胰岛素水平与β-肾上腺素能受体拮抗剂。具有和不具有内在拟交感活性的心脏选择性和非心脏选择性β-肾上腺素能受体拮抗剂对血糖正常犬基础胰岛素水平及葡萄糖刺激后胰岛素水平的影响。

Plasma insulin levels and beta-adrenoceptor antagonists. The effects of cardioselective and non-cardioselective beta-adrenoceptor antagonists with and without intrinsic sympathomimetic activity on basal insulin level and insulin level after glucose stimulation in normoglycemic dogs.

作者信息

Conca W, Beck A, Bacher S, Raberger G

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1982 Jul;320(1):63-6. doi: 10.1007/BF00499074.

Abstract

The effect of beta-adrenoceptor antagonists on the intravenous glucose tolerance test was investigated in conscious dogs. dl-Celiprolol (cardioselective with ISA = intrinsic sympathomimetic activity) 200 and 1000 microgram/kg i.v., dl-metoprolol (cardio-selective without ISA) 200 and 1000 microgram/kg i.v., dl-pindolol (non-selective with ISA) 5 and 25 microgram i.v. and l-bupranolol (non-selective without ISA) 10 and 50 microgram/kg i.v. were used in the study. The influence of beta-adrenoceptor antagonists on the plasma glucose and immunoreactive insulin following intravenous glucose tolerance test were evaluated by calculating the respective areas under the plasma curve. The present investigation clearly demonstrates the marked difference between the various beta-adrenoceptor antagonists on heart rate and, especially on metabolic parameters. dl-Metoprolol, a beta-adrenoceptor antagonist with cardioselectivity and without ISA can be assumed not to alter plasma insulin level and glucose assimilation. l-Bupranolol, a non-selective beta-adrenoceptor antagonist without ISA reduces plasma insulin level and probably enhances peripheral glucose uptake, resulting in an "unchanged" glucose tolerance. dl-Celiprolol or dl-pindolol, beta-adrenoceptor antagonists with ISA, but cardioselective or non-selective enhance both, basal insulin level and insulin level after glucose stimulation but must be assumed to decrease peripheral glucose uptake since here too glucose tolerance was unchanged.

摘要

在清醒犬中研究了β-肾上腺素受体拮抗剂对静脉葡萄糖耐量试验的影响。本研究使用了静脉注射剂量为200和1000微克/千克的dl-塞利洛尔(具有内在拟交感活性的心脏选择性药物)、静脉注射剂量为200和1000微克/千克的dl-美托洛尔(无内在拟交感活性的心脏选择性药物)、静脉注射剂量为5和25微克的dl-吲哚洛尔(具有内在拟交感活性的非选择性药物)以及静脉注射剂量为10和50微克/千克的l-布普洛尔(无内在拟交感活性的非选择性药物)。通过计算血浆曲线下的相应面积来评估β-肾上腺素受体拮抗剂对静脉葡萄糖耐量试验后血浆葡萄糖和免疫反应性胰岛素的影响。本研究清楚地表明了各种β-肾上腺素受体拮抗剂在心率尤其是代谢参数方面存在显著差异。可以认为,具有心脏选择性且无内在拟交感活性的β-肾上腺素受体拮抗剂dl-美托洛尔不会改变血浆胰岛素水平和葡萄糖同化作用。无内在拟交感活性的非选择性β-肾上腺素受体拮抗剂l-布普洛尔可降低血浆胰岛素水平,并可能增强外周葡萄糖摄取,从而导致葡萄糖耐量“不变”。具有内在拟交感活性的β-肾上腺素受体拮抗剂dl-塞利洛尔或dl-吲哚洛尔,无论是心脏选择性还是非选择性的,都会提高基础胰岛素水平以及葡萄糖刺激后的胰岛素水平,但由于葡萄糖耐量在此处同样未变,因此必须假定它们会降低外周葡萄糖摄取。

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