Basic pharmacological evaluation of modified phenyl carbamic acid derivatives on cardiovascular functions under in vitro conditions in rats.

IF 1.3 4区 生物学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY General physiology and biophysics Pub Date : 2025-01-01 DOI:10.4149/gpb_2024041
Eva Kralova, Ivan Malik
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Abstract

The study aimed to evaluate the basic pharmacological effects of modified phenyl carbamic acid derivates with a basic part made of N-phenylpiperazine (compounds 6a, 6b, 6c, 6d) in Wistar rats. The compounds were evaluated for their ability to decrease the phenylephrine-induced contraction of the aortic strips of rats after repeated administration of the compounds and their ability to inhibit the positive chronotropic effect of isoproterenol on spontaneously beating rat atria. The ability to inhibit the vasoconstriction effect of phenylephrine was confirmed in all compounds in the range from 10.39 % to 13.65 %. The most significant vasoconstriction was achieved in compound 6d (86.35%, p < 0.001). None of the compounds reached the effect of carvedilol. All compounds proved an antagonistic ability to the positive chronotropic effect of isoproterenol. The highest value of the anti-isoproterenol effect was identified for the compound 6c (pA2 = 8.21 ± 0.56; p < 0.05). Only compound 6a decreased heart rate significantly (by 3.17%, p < 0.05), so we can indicate its potential negative chronotropic effect. The obtained results showed that the evaluated compounds confirmed the basic characteristics of beta-blockers with additional α-adrenolytic properties.

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改性苯氨基甲酸衍生物在体外条件下对大鼠心血管功能的基础药理评价。
本研究旨在评价以n -苯基哌嗪(化合物6a、6b、6c、6d)为基部的改性苯基氨基甲酸衍生物对Wistar大鼠的基本药理作用。我们评估了这些化合物在反复给药后减少苯肾上腺素引起的大鼠主动脉条收缩的能力,以及它们抑制异丙肾上腺素对自发跳动的大鼠心房的正性变时作用的能力。苯肾上腺素对血管收缩的抑制作用在10.39% ~ 13.65%范围内得到证实。复合物6d血管收缩最明显(86.35%,p < 0.001)。没有一种化合物达到卡维地洛的效果。所有化合物均对异丙肾上腺素的正性变时作用有拮抗作用。抗异丙肾上腺素效果最高的是化合物6c (pA2 = 8.21±0.56;P < 0.05)。只有化合物6a显著降低心率(3.17%,p < 0.05),提示其可能具有负性变时作用。结果表明,所评价的化合物证实了β受体阻滞剂的基本特征,并具有额外的α-肾上腺素溶解特性。
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来源期刊
General physiology and biophysics
General physiology and biophysics 生物-生化与分子生物学
CiteScore
2.70
自引率
0.00%
发文量
42
审稿时长
6-12 weeks
期刊介绍: General Physiology and Biophysics is devoted to the publication of original research papers concerned with general physiology, biophysics and biochemistry at the cellular and molecular level and is published quarterly by the Institute of Molecular Physiology and Genetics, Slovak Academy of Sciences.
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