{"title":"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。","authors":"Eva Kralova, Ivan Malik","doi":"10.4149/gpb_2024041","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":12514,"journal":{"name":"General physiology and biophysics","volume":"44 1","pages":"73-79"},"PeriodicalIF":1.3000,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Basic pharmacological evaluation of modified phenyl carbamic acid derivatives on cardiovascular functions under in vitro conditions in rats.\",\"authors\":\"Eva Kralova, Ivan Malik\",\"doi\":\"10.4149/gpb_2024041\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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.</p>\",\"PeriodicalId\":12514,\"journal\":{\"name\":\"General physiology and biophysics\",\"volume\":\"44 1\",\"pages\":\"73-79\"},\"PeriodicalIF\":1.3000,\"publicationDate\":\"2025-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"General physiology and biophysics\",\"FirstCategoryId\":\"99\",\"ListUrlMain\":\"https://doi.org/10.4149/gpb_2024041\",\"RegionNum\":4,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"General physiology and biophysics","FirstCategoryId":"99","ListUrlMain":"https://doi.org/10.4149/gpb_2024041","RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
Basic pharmacological evaluation of modified phenyl carbamic acid derivatives on cardiovascular functions under in vitro conditions in rats.
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.
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.