Beta-1 Receptor (β1) in the Heart Specific Indicate to Stereoselectivity

Ayyad Rezk Rezk, Mansour Ahmed Mohamed, Nejm Ahmed Mohamed, Hassan Yasser Abdel Allem, Gabr Norhan Hassan, Ayyad Ahmed Rezk
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Abstract

The β1 receptor is one of the three beta receptors present in the human body, namely β1, β2, and β3. The β1 receptor is predominantly located in the heart, where it plays a crucial role in regulating the heart rate and the force of contraction, thereby increasing the cardiac output and the efficiency of blood pumping throughout the body. This receptor is targeted by a variety of pharmaceutical agents known as beta-blockers, which are commonly used in the treatment of cardiovascular conditions such as hypertension, angina, and arrhythmias.The β1 receptor exhibits stereoselectivity, meaning that different enantiomers (chiral molecules) of beta blockers can have varying levels of effectiveness and side effects. This study focuses on the stereoselectivity of the β1 receptor and the clinical implications of this property. It includes an examination of various β1 blockers, such as propranolol (a non-selective beta blocker), and selective β1 blockers like atenolol, bisoprolol, nebivolol, metoprolol, esmolol, acebutolol, and betaxolol. Each of these drugs has a unique chemical structure, with specific functional groups that contribute to their selective action on the β1 receptor. Furthermore, the β2 receptor, which is mainly present in the bronchi and bronchioles, is responsible for bronchodilation, and the β3 receptor, found in the bladder, helps reduce urinary urgency. Understanding the distinct locations and functions of these receptors allows for the development of targeted therapies with minimal off-target effects. This review highlights the importance of stereoselectivity in the development and use of β1 blockers, discussing their chemical structures, pharmacological activities, and therapeutic uses. It also explores the potential for future research and development of more selective and effective β1 receptor agonists and antagonists, which could offer improved therapeutic outcomes for patients with cardiovascular diseases. This study underscores the significant role of the β1 receptor in cardiovascular health and provides insights into the ongoing advancements in beta-blocker therapy. By delving into the stereoselectivity and specific actions of these drugs, the research aims to enhance the understanding and optimization of β1 receptor-targeted treatments in clinical practice.
心脏中的β1受体(β1)对立体选择性的特异性指示
β1受体是人体内存在的三种β受体(即β1、β2和β3)之一。β1 受体主要位于心脏,在调节心率和收缩力方面起着至关重要的作用,从而提高心输出量和全身血液泵送效率。β1受体具有立体选择性,这意味着不同对映体(手性分子)的β受体阻滞剂会产生不同程度的药效和副作用。本研究的重点是β1受体的立体选择性及其临床意义。它包括对各种 β1 受体阻滞剂(如普萘洛尔(一种非选择性β受体阻滞剂))和选择性 β1 受体阻滞剂(如阿替洛尔、比索洛尔、奈比洛尔、美托洛尔、艾司洛尔、醋丁洛尔和倍他洛尔)的研究。每种药物都有独特的化学结构和特定的功能基团,从而对 β1 受体产生选择性作用。此外,β2 受体主要存在于支气管和细支气管中,负责支气管扩张;β3 受体存在于膀胱中,有助于减轻尿急症状。了解了这些受体的不同位置和功能,就能开发出最小脱靶效应的靶向疗法。这篇综述强调了立体选择性在开发和使用 β1 受体阻断剂中的重要性,讨论了它们的化学结构、药理活性和治疗用途。它还探讨了未来研究和开发更具选择性和更有效的 β1 受体激动剂和拮抗剂的潜力,这些药物可改善心血管疾病患者的治疗效果。这项研究强调了β1受体在心血管健康中的重要作用,并为目前β-受体阻滞剂疗法的进展提供了启示。通过深入研究这些药物的立体选择性和特异性作用,该研究旨在加强临床实践中对β1受体靶向治疗的理解和优化。
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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