[The effects of compound IZ35 on the beta-adrenergic mediator system].

M Markov, D Zheliazkov, Ch Ivanov
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Abstract

The biological activity of the compound Iz35, representing rigid conformer of triquinol in respect to the cardiovascular system and smooth musculature, was studied. The arterial blood pressure and heart frequency were recorded in cats and rabbits as well as the tonus of smooth musculature of bronchial tree, uterus and intestines in experiments in vivo and in vitro of rats, guinea pigs and rabbits. It was established that the compound Iz35, administered in a wide range of doses of 0.1-5 mg/kg intravenously lowered systolic arterial blood pressure, but did not change chronotropic function of the heart (statistically significantly) in contrast to isoprenaline and thymolol. The compound Iz35 and trinquinol, administered intravenously in doses off 0.01-0.1 mg/kg, manifested broncholytic effect in experiments in vivo on various models of experimental bronchospasm of guinea pigs. They had still marked spasmolytic activity (1 x 10(-9)-1 x 10(-6) g/cm2 in respect to stomach-intestinal and uterine smooth musculature. The effects of Iz35 on the cardiovascular system and smooth musculature were inhibited considerably on the background of beta-adrenergic blockade (propranolol) in comparison with triquinol. The obtained data as well as our previous studies suggest to accept that these effects of the compound Iz35 are connected mainly with affecting beta-adrenergic mediator system and it manifests double agonistic/antagonistic activity in accordance with its dose characteristic.

[化合物IZ35对-肾上腺素能介质系统的影响]。
本文研究了三喹啉刚性构象化合物Iz35在心血管系统和平滑肌方面的生物活性。在大鼠、豚鼠、家兔的体内、体外实验中,记录猫、家兔的动脉血压、心跳频率以及支气管树、子宫、肠的平滑肌张力。结果表明,与异丙肾上腺素和百里香酚相比,化合物Iz35在0.1-5 mg/kg的大剂量范围内静脉注射可降低动脉收缩压,但不改变心脏的变时功能(统计学意义显著)。以0.01 ~ 0.1 mg/kg剂量静脉给药的化合物Iz35和三苯甲醇对豚鼠各种实验性支气管痉挛模型均有溶支作用。它们仍有明显的解痉活性(1 × 10(-9)-1 × 10(-6) g/cm2)。与triquinol相比,在β -肾上腺素能阻断剂(心得安)的背景下,Iz35对心血管系统和平滑肌的作用明显受到抑制。所得数据和我们之前的研究表明,化合物Iz35的这些作用主要与影响β -肾上腺素能介质系统有关,并根据其剂量特性表现出双重激动/拮抗活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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