• blood vessels
  • ET A receptors are found in the medial smooth muscle layers of the blood vessels, and atrial and ventricular myocardium. (ahajournals.org)
  • 11 This agrees with the prior demonstration of normal or only slightly depressed responses to ET-1 and the absence of important downregulation of endothelin receptors in blood vessels or smooth muscle cells of SHR. (ahajournals.org)
  • There are at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC, all of which are G protein-coupled receptors whose activation result in elevation of intracellular-free calcium, which constricts the smooth muscles of the blood vessels, raising blood pressure, or relaxes the smooth muscles of the blood vessels, lowering blood pressure, among other functions. (wikipedia.org)
  • Widely distributed in the body, receptors for endothelin are present in blood vessels and cells of the brain, choroid plexus and peripheral nerves. (wikipedia.org)
  • affinity
  • It has the same affinity at the ET B receptor as ET-1 but, at physiological concentrations, has little or no affinity for the ET A . The only endogenous peptides with a high degree of sequence similarity to the ETs are the sarafotoxins (S6a, S6b, S6c, S6d). (guidetopharmacology.org)
  • It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2. (curehunter.com)
  • ETB receptors bind ETs and SRTXs with little selectivity whereas ETA receptors show greater affinity for ET-1, ET-2 and SRTX-b, over ET-3 and SRTX-c. (wikipedia.org)
  • Although ACT-132577 has a lower affinity for the ET receptors than its parent compound, It maintains higher plasma concentrations than macitentan. (wikipedia.org)
  • pulmonary
  • ET receptor antagonism has been demonstrated to be beneficial in patients with pulmonary hypertension. (ahajournals.org)
  • The selective ET A receptor antagonist sitaxsentan also improves hemodynamics and exercise capacity in patients with pulmonary arterial hypertension. (ahajournals.org)
  • This chapter provides an overview of the endothelin system as well as preclinical data of ERA studies obtained in disease models of arterial hypertension, atherosclerosis, coronary artery disease, pulmonary hypertension, heart failure, renal disease, and allograft rejection following cardiac transplantation. (springer.com)
  • Pulmonary Actions of the Endothelins. (wikipedia.org)
  • Macitentan (trade name Opsumit) is an endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH). (wikipedia.org)
  • peptides
  • The main differences in the family of endothelin and sarafotoxins appear at N-terminal of peptides, as C-terminal in all of them is almost the same. (wikipedia.org)
  • Clinical
  • The Swiss affiliate is located in Baden, the German affiliate in Freiburg, the Austrian one in Vienna, the French one in Paris and the UK affiliate is located in London In 2006, the company established the Actelion Endothelin Research Award programme which supports selected clinical research projects. (wikipedia.org)