Evaluation of the antagonistic effect of pyrimidinone-containing compounds on alpha-adrenergic receptors: candidates for antihypertensive drugs

Evaluation of the antagonistic effect of pyrimidinone-containing compounds on alpha-adrenergic receptors: candidates for antihypertensive drugs

• Autor
• Ruth Cristina Albuquerque Santos
• Co-autores
• Sidiane Barros da Silva , Silvia Maria de Luna Alves , Alice Valença Araújo
• Resumo

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  Introduction: Chronic Noncommunicable Diseases (CNCD) includes cardiovascular diseases (CVD), diabetes, cancer and chronic respiratory disease. Among them, CVDs are responsible for the highest percentage of deaths in the world and Systemic Arterial Hypertension is the most important risk factor for their development. Different classes of antihypertensive drugs are available in Brazil, including ?1-adrenergic receptor antagonists. However, the existing drugs are not very selective, as well as induce adverse effects. Objective: To evaluate the activity of new molecules containing the pyrimidinone ring on ?1-adrenergic receptors in isolated aorta from rats. Method: Vascular reactivity experiments will be carried out on male Wistar rats (2-3 months old). The thoracic aortic artery will be isolated and the connective tissues and fat will be removed. 4 mm long rings will be mounted between two stainless steel stirrups, one of which is connected to a force transducer to record the isometric tension. Cumulative concentration-effect curves for phenylephrine and KCl will be performed in the absence or in the presence of different concentrations of the molecules (1, 10 e 100 mmol/L). Prazosin will be used as a positive control. From the concentration-effect curves obtained, it will be calculated the maximum effect (Emax) and pD2. Statistical analyzes will be performed by using the GraphPad Prism©. The differences among groups will be verified by Student's t test or one-way analysis of variance (ANOVA). This study was submitted to Animal Use Ethics Committee of the Federal University of Pernambuco (0072/2020). Expected Results: It is expected to characterize the action of new alpha-adrenergic receptor antagonists, making such compounds candidates for antihypertensive drug.

   

• Palavras-chave
• Adrenoceptors, hypertension, vascular reactivity
• Modalidade
• Comunicação oral
• Área Temática
• Revisões, projetos, revisões sistemáticas e metanálises em biologia vascular