Evaluation of Biological Activity Exerted by Dibenzo[b,e]Thiophene-11(6H)-One on Left Ventricular Pressure Using an Isolated Rat Heart Model.

IF 1.7 Q3 PHARMACOLOGY & PHARMACY Drug Research Pub Date : 2023-06-01 DOI:10.1055/a-1995-6351

Lauro Figueroa-Valverde, Marcela Rosas-Nexticapa, Magdalena Alvarez-Ramirez, Maria López-Ramos, Francisco Díaz-Cedillo, Maria Virginia Mateu-Armad

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引用次数: 2

Abstract

Background: Some studies show that some Dibenzo derivatives can produce changes in the cardiovascular system; however, its molecular mechanism is not very clear.

Objective: The objective of this investigation was to evaluate the inotropic activity of ten Dibenzo derivatives (compounds 1 to 10) on either perfusion pressure or left ventricular pressure.

Methods: Biological activity produced by the Dibenzo derivatives on either perfusion pressure or coronary resistance was evaluated using an isolated rat heart. In addition, the molecular mechanism of biological activity produced by compound 4 (Dibenzo[b,e]thiophene-11(6H)-one) on left ventricular pressure was determined using both Bay-k8644 and nifedipine as pharmacological tools in an isolated rat heart model.

Results: The results showed that Dibenzo[b,e]thiophene-11(6H)-one increases perfusion pressure and coronary resistance at a dose of 0.001 nM. Besides, other data display that Dibenzo[b,e]thiophene-11(6H)-one increases left ventricular pressure in a dose-dependent manner (0.001 to 100 nM) and this effect was similar to biological activity produced by Bay-k8644 drug on left ventricular pressure. However, the effect exerted by Dibenzo[b,e]thiophene-11(6H)-one was inhibited in the presence of nifedipine at a dose of 1 nM.

Conclusions: All these data suggest that Dibenzo[b,e]thiophene-11(6H)-one increase left ventricular pressure through calcium channel activation. In this way, Dibenzo[b,e]thiophene-11(6H)-one could be a good candidate as positive inotropic agent to heart failure.

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用离体大鼠心脏模型评价二苯并[b,e]噻吩-11(6H)- 1对左心室压力的生物活性

背景:一些研究表明，某些二苯并衍生物可以引起心血管系统的变化;然而，其分子机制尚不清楚。目的:本研究的目的是评价十种二苯并衍生物(化合物1 ~ 10)对灌注压或左心室压的肌力活性。方法:用离体大鼠心脏评价二苯并衍生物对灌注压和冠状动脉阻力的生物活性。此外，在离体大鼠心脏模型中，以Bay-k8644和硝苯地平为药理学工具，确定化合物4(二苯并[b,e]噻吩-11(6H)- 1)对左心室压力产生生物活性的分子机制。结果:结果显示，二苯并[b,e]噻吩-11(6H)- 1在0.001 nM剂量下可增加灌注压和冠状动脉阻力。此外，其他数据显示，二苯并[b,e]噻吩-11(6H)- 1以剂量依赖的方式增加左心室压力(0.001 ~ 100 nM)，这种作用与Bay-k8644药物对左心室压力产生的生物活性相似。然而，二苯并[b,e]噻吩-11(6H)- 1的作用在1 nM硝苯地平的存在下被抑制。结论:以上数据提示二苯并[b,e]噻吩-11(6H)- 1通过激活钙通道增加左室压。因此，二苯并[b,e]噻吩-11(6H)- 1可能是治疗心力衰竭的正性肌力药物。

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来源期刊

Drug Research PHARMACOLOGY & PHARMACY-

CiteScore

3.50

自引率

0.00%

发文量

期刊介绍： Drug Research (formerly Arzneimittelforschung) is an international peer-reviewed journal with expedited processing times presenting the very latest research results related to novel and established drug molecules and the evaluation of new drug development. A key focus of the publication is translational medicine and the application of biological discoveries in the development of drugs for use in the clinical environment. Articles and experimental data from across the field of drug research address not only the issue of drug discovery, but also the mathematical and statistical methods for evaluating results from industrial investigations and clinical trials. Publishing twelve times a year, Drug Research includes original research articles as well as reviews, commentaries and short communications in the following areas: analytics applied to clinical trials chemistry and biochemistry clinical and experimental pharmacology drug interactions efficacy testing pharmacodynamics pharmacokinetics teratology toxicology.