Kowalczyk Agata, Kołodziejczyk Michał, Gorąca Anna
Zakład Fizjologii Układu Krążenia, Międzywydziałowa Katedra Fizjologii Doświadczalnej i Klinicznej, Uniwersytet Medyczny w Łodzi.
Zakład Technologii Postaci Leku, Katedra Farmacji Stosowanej, Uniwersytet Medyczny w Łodzi.
Postepy Hig Med Dosw (Online). 2014 Jan 2;68:1076-80. doi: 10.5604/17322693.1119730.
Endothelins are endothelial peptides, the properties of which have been investigated for over 25 years. They play a special role in the pathophysiology of many diseases of the cardiovascular system. Endothelin-1, which is the most explored one, is a potent vasoconstrictor. It increases renal water and sodium excretion, augments cell growth and proliferation and has proinflammatory activity, by intensifying the production of reactive oxygen and nitrogen species (ROS and RNS). ET-1 takes part in the progression of such diseases as hypertension, atherosclerosis, heart and renal failure. The physio- and pathological effects of endothelins are mediated through ETA and ETB receptors. Blocking these receptors, in particular the ETA receptor, can prevent negative effects of endothelins. Long-term efforts to create drugs which act like that have brought relevant results. Endothelin receptor antagonists (ERA) are a new class of medicines, which are indicated in the treatment of pulmonary arterial hypertension. There are also optimistic results of trials with ERA administered in other disorders. On the basis of these data we may conclude that there will be more indications for this group of drugs. This review discusses properties and new research directions of ERA registered in pharmacotherapy.
内皮素是内皮肽,其特性已被研究了25年以上。它们在许多心血管系统疾病的病理生理学中发挥着特殊作用。内皮素-1是研究最多的一种,是一种强效血管收缩剂。它可增加肾脏水和钠的排泄,促进细胞生长和增殖,并通过增强活性氧和氮物质(ROS和RNS)的产生而具有促炎活性。ET-1参与高血压、动脉粥样硬化、心脏和肾衰竭等疾病的进展。内皮素的生理和病理作用是通过ETA和ETB受体介导的。阻断这些受体,尤其是ETA受体,可以预防内皮素的负面影响。长期致力于研发此类药物已取得了相关成果。内皮素受体拮抗剂(ERA)是一类新型药物,被用于治疗肺动脉高压。在其他疾病中使用ERA进行试验也取得了乐观的结果。基于这些数据,我们可以得出结论,这类药物将会有更多的适应证。本综述讨论了药物治疗中注册的ERA的特性和新的研究方向。