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基于猫和大鼠的一些代谢反应对2-氨基四氢萘新衍生物的β-肾上腺素能阻断活性研究

Beta-adrenoblocking activity of a new derivative of 2-aminotetraline based on some metabolic responses in cats and rats.

作者信息

Bogoslovova T, Staneva-Stoytcheva D

机构信息

Department of Experimental Pharmacology and Toxicology, Institute of Pharmacology and Pharmacy, Medical Academy, Sofia.

出版信息

Acta Physiol Pharmacol Bulg. 1988;14(3):39-45.

PMID:2906208
Abstract

Previous pharmacological investigations of a newly synthetized derivative of 2-aminotetraline: trans-2-isopropylamino-3-hydroxy-5,8-dimethoxy 1,2,3,4-tetrahydronaphthalene (3b) have shown it to possess a beta-adrenergic blocking activity. In the present work we studied the influence of 3b on some biochemical indices characteristic of beta-adrenergic stimulation: blood levels of glucose, lactate and FFA in cats and rats, and phosphorylase "a" activity in rat myocardium. The dose used (0.5 mg/kg) in rats was the same as the dose of propranolol (0.5 mg/kg). In all experiments on cats and rats compound 3b decreased the effects of isoproterenol on the blood levels of glucose, lactate and FFA and on the phosphorylase "a" activity of the myocardium and this action was comparable with that of propranolol. The similar molecular mass and LD50 of 3b and propranolol allowed quantitative comparisons of the beta-adrenoblocking effects of both drugs in the dose used. The results suggest that compound 3b possesses metabolic effects characteristic of beta-adrenoblocking agents.

摘要

先前对新合成的2-氨基四氢萘衍生物:反式-2-异丙基氨基-3-羟基-5,8-二甲氧基-1,2,3,4-四氢萘(3b)的药理学研究表明,它具有β-肾上腺素能阻断活性。在本研究中,我们研究了3b对β-肾上腺素能刺激的一些生化指标的影响:猫和大鼠的血糖、乳酸和游离脂肪酸水平,以及大鼠心肌中的磷酸化酶“a”活性。大鼠使用的剂量(0.5mg/kg)与普萘洛尔的剂量(0.5mg/kg)相同。在所有对猫和大鼠的实验中,化合物3b均降低了异丙肾上腺素对血糖、乳酸和游离脂肪酸水平以及心肌磷酸化酶“a”活性的影响,且该作用与普萘洛尔相当。3b和普萘洛尔相似的分子量和半数致死量使得能够对两种药物在所使用剂量下的β-肾上腺素能阻断作用进行定量比较。结果表明,化合物3b具有β-肾上腺素能阻断剂的代谢效应。

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