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.
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http://dx.doi.org/10.5604/17322693.1119730 | DOI Listing |
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Dr. Babasaheb Ambedkar Technological University, Lonere, Raigad, 402103, India.
Acute lung injury i.e. ALI and its serious form acute respiratory distress syndrome (ARDS) are incurable medical conditions associated with significant global mortality and morbidity.
View Article and Find Full Text PDFNeurosurg Rev
January 2025
Dow Medical College, Dow University of Health Sciences, Karachi, Pakistan.
Aneurysmal Subarachnoid Hemorrhage (aSAH), resulting from ruptured aneurysms, is a major contributor to stroke-related mortality and morbidity. Despite advances in healthcare, aSAH remains severe and often leads to complications such as cerebral vasospasm (CV), cerebral infarction, and delayed ischemic neurological deficits (DIND). Clazosentan, an endothelin receptor antagonist, has demonstrated potential in alleviating vasospasm and its associated outcomes, although evidence of its efficacy remains unclear.
View Article and Find Full Text PDFAlzheimers Dement
December 2024
Centre for Brain Research, Indian Institute of Science, Bengaluru, Karnataka, India.
Background: Vascular pathology is often seen in cases of mixed dementia affecting elderly population including Alzheimer's disease (AD). AD is generally characterized by the presence of amyloid-β (Aβ) plaques and tau deposits. However, many factors influence the onset and progression of AD pathology.
View Article and Find Full Text PDFSci Rep
January 2025
Institute of Human Genetics, Polish Academy of Sciences, Strzeszynska 32, Poznan, 60-479, Poland.
Despite advances in neonatal and ophthalmological care, retinopathy of prematurity (ROP) continues to be a leading cause of childhood blindness worldwide. Investigating gene variants associated with vascular responses in ROP may provide valuable insights into its pathogenesis and identify risk or protective factors. Nitric oxide (NO) and endothelin-1 (ET-1) play roles in vascular regulation, influencing processes relevant to ROP development.
View Article and Find Full Text PDFRegul Toxicol Pharmacol
December 2024
Division of Nephrology, University of Utah Health, Salt Lake City, UT, USA.
Marketed endothelin receptor antagonists (ERAs) have been associated with testicular tubular atrophy and decreases in male animal fertility in chronic toxicity studies in rats and dogs. Consistent with these findings, reduced sperm count has been observed in the clinical setting and is considered a potential class risk with chronic administration of ERAs. In contrast, no such effects on male animal fertility are noted with angiotensin II type 1 receptor blocker (ARB) treatment.
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