ReceptorsPeptidesBosentanAngiotensinVascularAntagonistsReceptor type2023PotentPeptideEnzymePathophysiology1995ExtracellularEndothelial dysfunctionNeuronsSubstancesRenalConcentrationsContractionBasic and clinicalCardiacVentricularSerumStimuliEffectsNitricStimulatesDegradationAortaPodocytesSensitivityPulmonary arterialIsolationMeSHKidneyElevationAccumulationCardiovascularGeneRolesCellRole
Receptors22
- Endothelins are peptides with receptors and effects in many body organs. (wikipedia.org)
- Endothelin functions through activation of two G protein-coupled receptors, endothelinA and endothelinB receptor (ETA and ETB, respectively). (wikipedia.org)
- Most endothelin receptors in the human cerebral cortex (~90%) are of the ETB subtype. (wikipedia.org)
- Endothelin-2 differs from endothelin-1 by two amino acids, and sometimes has the same affinity as endothelin-1 for ETA and ETB receptors. (wikipedia.org)
- Endothelin receptors are present in the three pituitary lobes which display increased metabolic activity when exposed to ET-1 in the blood or ventricular system. (wikipedia.org)
- The ubiquitous distribution of endothelin peptides and receptors implicates involvement in a wide variety of physiological and pathological processes among different organ systems. (wikipedia.org)
- Receptors for endothelin-1 exist in brain neurons, indicating a potential role in neural functions. (wikipedia.org)
- Tumours of the Ewing's sarcoma (ES) family and neuroblastoma (NBL) were examined by reverse transcriptase-PCR for expression of mRNA for endothelin (ET) receptors ET-A and ET-B, and the ligands ET-1, ET-2 and ET-3. (portlandpress.com)
- These agents competitively bind to endothelin-1 (ET-1) receptors ET A and ET B in endothelium and vascular smooth muscle, inhibiting vessel constriction and elevation of blood pressure. (medscape.com)
- Endothelin (16-21) is a full agonist at ET-B receptros, but is inactive or weakly active at ET-A receptors. (peptide.com)
- Endothelins action on ETA and ETB receptors (ETARs and ETBRs) [6 7 both G protein-coupled receptors that may activate multiple G proteins types and impact several signaling pathways [8]. (exposed-skin-care.net)
- Results Endothelin receptors in dorsal root ganglion neurons The expression of endothelin receptor subtypes in the rat lumbar DRG was analyzed in binding experiments using 125I-ET-1 as the radioligand. (exposed-skin-care.net)
- The endothelin-1-mediated spontaneous Ca 2+ transients were abolished by application of 2-aminoethoxydiphenyl borate (2-APB), an antagonist of Ins(1,4,5) P 3 receptors. (biologists.com)
- Sandhu, H, Xu, C-B & Edvinsson, L 2009, ' DMSO-Lipid Soluble Cigarette Smoking Particles Upregulate Contractile Endothelin Type B And Thromboxane A2 Receptors Of Rat Middle Cerebral Arteries ', Hypertension , vol. 54, no. 5, pp. 1175-1176. (lu.se)
- More than 35 years ago the Japanese physician-scientist Tomoh Masaki (1934-2020) discovered endothelins and endothelin receptors at the University of Tsukuba between 1987 and 1990. (endothelins.com)
- This large body of evidence demonstrates the antitumor activity of endothelin receptor antagonists and provides a rationale for the clinical evaluation of these molecules alone and in combination with cytotoxic drugs or molecular inhibitors leading to a new generation of anticancer therapies targeting endothelin receptors. (biomedcentral.com)
- Endothelins exert their effects by binding to two distinct cell surface ET receptors, ET A and ET B . The ET B receptor (ET B R) binds the three peptide isotypes with equal affinity. (biomedcentral.com)
- Endothelin receptor antagonists bind endothelin 1 receptors, causing a decrease in pulmonary arterial pressure through decreases in PVR. (medscape.com)
- Endothelin and its receptors are very highly expressed in the kidney. (medtelligence.net)
- The action of endothelin is mediated through binding of two receptors ETA and ETB. (elisakits.co.uk)
- Conversion of big endothelin-1 in rat uterus causes contraction mediated by ETA receptors. (elisakits.co.uk)
- Gα12/13 are expressed in podocytes and couple to angiotensin II, thrombin, endothelin and LPA receptors, which are important in renal injury. (medscape.com)
Peptides5
- Endothelins are 21-amino acid vasoconstricting peptides produced primarily in the endothelium having a key role in vascular homeostasis. (wikipedia.org)
- These two subtypes of endothelin receptor are distinguished in the laboratory by the order of their affinity for the three endothelin peptides: the ETA receptor is selective for ET-1, whereas the ETB receptor has the same affinity for all three ET peptides. (wikipedia.org)
- The endothelins ET-1 ET-2 and ET-3 are vasoactive peptides originally cloned from endothelial cells [1] but also made by various other cell types including Taladegib some tumor cells [2-5]. (exposed-skin-care.net)
- Endothelins (ET) are 21 amino acid vasoactive peptides, which have 3 forms in most mammals (ET-1, ET-2, ET-3). (huveta.hu)
- The endothelins, that includes three 21-aa peptides ET-1, ET-2 and ET-3, are potent vasoconstricting peptides, involved in the pathophysiology of different malignancies [ 1 , 2 ]. (biomedcentral.com)
Bosentan4
- Overproduction of endothelin in the lungs may cause pulmonary hypertension, which was treatable in preliminary research by bosentan, sitaxentan or ambrisentan. (wikipedia.org)
- Bosentan is an endothelin receptor antagonist indicated for the treatment of pulmonary arterial hypertension (PAH) in patients with WHO class III or IV symptoms. (medscape.com)
- Scholars@Duke publication: Bosentan, an endothelin antagonist, augments hepatic graft function by reducing graft circulatory impairment following ischemia/reperfusion injury. (duke.edu)
- Bosentan, a novel endothelin receptor antagonist, was infused directly into the portal vein prior to cold ischemia and immediately on reperfusion, in five porcine livers. (duke.edu)
Angiotensin2
- Endothelin and angiotensin II stimulation of Na+-H+ exchange is impaired in cardiac hypertrophy. (jci.org)
- For example, both proteinuria and angiotensin stimulate renal endothelin production, while endothelin in turn can increase proteinuria and angiotensin. (medtelligence.net)
Vascular11
- Endothelin-1 is the most powerful endogenous chemical affecting vascular tone across organ systems. (wikipedia.org)
- Secretion of endothelin-1 from the vascular endothelium signals vasoconstriction and influences local cellular growth and survival. (wikipedia.org)
- Vascular dilatation is critically impaired in many diseases and is encountered by an upregulated endothelin receptor A (ETA) in the vasculature in association with a decline in nitric oxide bioavailability. (nih.gov)
- Endothelin receptor antagonist CPU0213 and ingredients from plant origins such as CPU86017, p-benzyl-tetra-hydro-berberine are effective in attenuating vascular abnormality by normalizing changes of biomarkers in the vascular wall. (nih.gov)
- One may speculate that, early after the development of RVO, systemic ET-1 level may increase, then decrease later till the onset of retinal neovascularisation, which might induce an increase again possibly via an increased expression of vascular endothelial growth factor (VEGF), since VEGF can cause an increased expression of endothelin converting enzyme. (bmj.com)
- Endothelin, a vasoconstrictor peptide secreted from endothelial cells, has been thought to play a role in various forms of vascular disease. (diabetesjournals.org)
- In addition to these functions, it modulates vascular tone by synthesizing and releasing a number of vasoactive factors that may have vasodilatory effects, such as nitric oxide (NO), prostacyclin (PGI 2 ), and endothelium-derived hyperpolarizing factor, and vasoconstrictor effects, such as thromboxane A 2 and endothelin-1 (ET-1) [ 8 ] . (encyclopedia.pub)
- Endothelin 1 is a potent endogenous vasoconstrictor that causes vascular smooth muscle hyperplasia in addition to direct vasoconstrictor effects. (medscape.com)
- Big endothelin-1 (ET-1) is synthesised and secreted from the vascular smooth muscle cells and endothelium, an inactive 39 amino acid peptide. (elisakits.co.uk)
- Vascular parameters and endothelin-1 measurements in glaucoma patients with low- and high-tension optic disc hemorrhages. (bvsalud.org)
- This prospective study aimed to compare vascular parameters ( endothelin-1 [ET-1] blood levels, laser Doppler imaging [LDI] of distal phalanxes, and nailfold capillaroscopy ) between open-angle glaucoma patients with low- and high-tension optic disc hemorrhages (LTDH and HTDH, respectively). (bvsalud.org)
Antagonists3
- Endothelin receptor antagonists (ERAs) are an important part of PAH therapy, with two ERAs currently approved for the treatment of PAH and a novel ERA that has recently been investigated in a Phase III clinical trial. (nih.gov)
- The endothelin conferences are held biannually in a rotating fashion in America, Europe, and Asia, presenting the latest in basic and clinical science on endothelins and endothelin receptor antagonists (ERAs). (endothelins.com)
- So now let's focus on the mechanism of action of endothelin antagonists because these agents promise to give us a new treatment option for the management of both of these conditions. (medtelligence.net)
Receptor type1
- Endothelin receptor type A signals both the accumulation of inositol phosphates and the inhibition of cyclic AMP generation in rat myometrium: stimulation and desensitization. (aspetjournals.org)
20232
- The «Eighteenth International Conference on Endothelin» (ET-18) will be held October 11-14, 2023, in Rome, Italy and co-chaired by Carmine Cardillo, Francesca Schinzari, and Neeraj "Bean" Dhaun. (endothelins.com)
- Endothelin-1 and Hypertension" Encyclopedia , https://encyclopedia.pub/entry/14671 (accessed November 30, 2023). (encyclopedia.pub)
Potent5
- Endothelins are the most potent vasoconstrictors known. (wikipedia.org)
- OBJECTIVES: Endothelin 1 (ET1) is one of a newly discovered family of potent naturally occurring vasoconstrictors produced by the endothelium. (bmj.com)
- This gene encodes the receptor for endothelin-1, a peptide that plays a role in potent and long-lasting vasoconstriction. (thermofisher.com)
- Endothelin-1 (ET-1) is a potent endogenous vasoconstrictor that also has the ability to induce a burning, non-histaminergic pruritus when exogenously administered, by activating the endothelin A receptor (ETR) on primary afferents. (iasp-pain.org)
- Endothelin is a potent hepatic vasoconstrictor. (duke.edu)
Peptide2
- Serum concentrations of the 21 amino acid peptide endothelin ET1-21 were measured by radioimmunoassay. (bmj.com)
- Chronic heart failure (CHF) studies investigating the clinical, hemodynamic, and therapeutic importance of endothelin-1 (ET-1), atrial natriuretic peptide (ANP), and brain natriuretic peptide (BNP) are largely based on resting plasma levels, which may vary with prior exertion and postprandial status. (uea.ac.uk)
Enzyme3
- Characterization of endothelin-converting enzyme from endothelial cells and rat brain: detection of the formation of biologically active endothelin-1 by rapid bioassay. (aspetjournals.org)
- These results show the presence of at least two different endothelin-converting enzyme activities in endothelial cells and a third within the rat brain. (aspetjournals.org)
- Conversion of big ET-1 in the rat lung: role of phosphoramidon-sensitive endothelin-1-converting enzyme. (elisakits.co.uk)
Pathophysiology2
- Studies have shown that endothelin-2 plays a significant role in ovarian physiology and could impact the pathophysiology of heart failure, immunology, and cancer. (wikipedia.org)
- Endothelin also directly stimulates mesangial cell proliferation, contraction, and extracellular matrix production-effects that are important in the pathophysiology of IgAN. (medtelligence.net)
19951
- 1995 ) Association of endothelin-1 with normal tension glaucoma: clinical and fundamental studies. (bmj.com)
Extracellular2
- Pertussis toxin preincubation followed by removal of extracellular calcium reduced further the endothelin responses by similar amounts in SHR and WKY cells, but SHR stimulated IP formation remained significantly decreased compared to WKY. (strath.ac.uk)
- It was concluded that SHR cells do not appear to have an alteration in endothelin-1 activated, pertussis toxin sensitive G-protein coupling to IP formation or in the dependence of inositol phosphate formation on extracellular calcium. (strath.ac.uk)
Endothelial dysfunction1
- The binding of platelets to the endothelial cell receptor LOX-1 causes a release of endothelin, which induces endothelial dysfunction. (wikipedia.org)
Neurons1
- Background Endothelin-1 (ET-1) both stimulates nociceptors and sensitizes these to noxious stimuli an impact probably mediated with the ETA receptor (ETAR) expressed in sensory neurons. (exposed-skin-care.net)
Substances1
- The aim of this study was to determine the involvement of vasoactive substances endothelin-1 (ET-1) and nitric oxide (NO) during early chronic CRPS1. (biomedcentral.com)
Renal3
- Renal endothelin expression is increased in almost all forms of kidney disease. (medtelligence.net)
- Many factors increase renal endothelin production and some can even form a vicious cycle. (medtelligence.net)
- And one of the questions I have is does endothelin act primarily on the renal vasculature? (medtelligence.net)
Concentrations4
- Serum endothelin concentrations in workers exposed to vibration. (bmj.com)
- The aim of this study was to compare serum endothelin concentrations in people with vibration induced white finger (VWF) with those of controls exposed to vibration, and unexposed (pure) controls. (bmj.com)
- Rapid increase in plasma endothelin concentrations during percutaneous balloon dilatation of the mitral valve in patients with mitral stenosis. (bmj.com)
- Cardiopulmonary and clinicopathologic variables, cytokine activity, and endothelin (ET) concentrations were recorded. (avma.org)
Contraction3
- We compared the effects of endothelin-1 (ET-1) on intracellular pH, intracellular [Ca2+]i, and cell contraction in hypertrophied adult ventricular myocytes from ascending aortic banded rats and age-matched controls. (jci.org)
- In estradiol-dominated rat myometrium, endothelin (ET)-1 caused contraction and increased the accumulation of [3H]inositol phosphates (EC50 = 70 nM), with the sequential generation of inositol trisphosphate, inositol bisphosphate, and inositol monophosphate. (aspetjournals.org)
- In rat aorta, endothelin-1 (ET-1) induced a slowly developing and sustained contraction in Ca(2+)-containing normal Krebs, nominally Ca(2+)-free Krebs, and Ca(2+)-free Krebs containing EGTA with a decreasing level of contraction. (mcmaster.ca)
Basic and clinical1
- As of 2018, endothelins remain under extensive basic and clinical research to define their roles in several organ systems. (wikipedia.org)
Cardiac2
- Among numerous diseases potentially occurring from endothelin dysregulation are: several types of cancer cerebral vasospasm following subarachnoid hemorrhage arterial hypertension, pulmonary hypertension, and other cardiovascular disorders pain mediation cardiac hypertrophy and heart failure Dengue haemorrhagic fever Type II diabetes some cases of Hirschsprung disease In insulin resistance the high levels of blood insulin results in increased production and activity of ET-1, which promotes vasoconstriction and elevates blood pressure. (wikipedia.org)
- Effects of exogenous big endothelin-1 on postischemic cardiac dysfunction and norepinephrine overflow in rat hearts. (elisakits.co.uk)
Ventricular3
- Incubation of electrically-paced ventricular myocytes with a membrane-permeant Ins(1,4,5) P 3 ester provoked the occurrence of spontaneous diastolic Ca 2+ transients with the same characteristics and sensitivity to 2-APB as the events stimulated by endothelin-1. (biologists.com)
- Regulation of phospholipases C and D in rat ventricular myocytes: stimulation by endothelin-1, bradykinin and phenylephrine. (reading.ac.uk)
- We have measured activation of these phospholipases by endothelin-1 (ET-1), bradykinin (BK), or phenylephrine (PE) in ventricular myocytes cultured from neonatal rat. (reading.ac.uk)
Serum2
- Rat big endothelin-1 ELISA kit is intended for analysing quantitative concentration of rat big ET-1 (big endothelin-1) in samples of cell culture supernatant, tissue extracts, serum and plasma. (elisakits.co.uk)
- There was a trend for increased serum endothelin-1. (cdc.gov)
Stimuli2
- Background Endothelin is certainly among the many regional mediators that are essential in pain era as well as the modulation of nociceptor responsiveness to unpleasant stimuli. (exposed-skin-care.net)
- The effects of endothelin-1 were compared with two other stimuli, isoproterenol and digoxin, which are known to induce inotropy and spontaneous Ca 2+ transients by overloading intracellular Ca 2+ stores. (biologists.com)
Effects5
- In preliminary research, injection of endothelin-1 into a lateral cerebral ventricle was shown to potently stimulate glucose metabolism in specified interconnected circuits of the brain, and to induce convulsions, indicating its potential for diverse neural effects in conditions such as epilepsy. (wikipedia.org)
- Both effects of endothelin-1 were blocked by an antagonist of phospholipase C, suggesting that Ins(1,4,5) P 3 and/or diacylglycerol production was necessary. (biologists.com)
- The effects of pertussis toxin on endothelin-1 and noradrenaline coupling to inositol phosphate (IP) formation was investigated in cultured aortic smooth muscle cells from 14 week SHR and WKY rats. (strath.ac.uk)
- In general though, endothelin can elicit a wide range of pathophysiological effects leading to things like cell proliferation, apoptosis, inflammation and fibrosis. (medtelligence.net)
- I think most importantly, these effects are largely mediated by activation of the endothelin A receptor. (medtelligence.net)
Nitric1
- Three pathways have been identified in the pathogenesis of pulmonary arterial hypertension (PAH): the endothelin (ET), nitric oxide (NO) and prostacyclin pathways. (nih.gov)
Stimulates1
- Endothelin preferentially stimulates efferent arteriolar constriction, thereby increasing interglomerular pressure. (medtelligence.net)
Degradation1
- Phosphoramidon-sensitive conversion of big endothelin-1 and degradation of endothelin-1 in rat kidney. (elisakits.co.uk)
Aorta1
- Atherosclerosis progression in the aorta was determined by the en face method. (cdc.gov)
Podocytes1
- Endothelin also directly acts on podocytes, where it can promote slit diaphragm and cytoskeletal disruption, podocyte loss, and proteinuria-actions that characterize FSGS. (medtelligence.net)
Sensitivity1
- The minimum sensitivity detection limit of big ET-1 using current rat big endothelin-1 ELISA kit was approximately 0.69 pg/ml. (elisakits.co.uk)
Pulmonary arterial1
- Endothelin concentration was increased in jugular venous and pulmonary arterial plasma in horses receiving LPS and ATP-MgCl 2 . (avma.org)
Isolation1
- Endothelins derived the name from their isolation in cultured endothelial cells. (wikipedia.org)
MeSH1
- Endothelin-Converting Enzymes" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (jefferson.edu)
Kidney1
- First, endothelin is produced by and acts upon virtually every cell type in the kidney. (medtelligence.net)
Elevation1
- Using the endothelin-1 (ET-1)-stimulated elevation in cGMP in LLC-PK1 cells as a biological detector system for the conversion of big ET-1 (bET-1) to ET-1, we detected bET-1-converting activities in subcellular fractions from bovine aortic cultured endothelial cells (BAE) and rat brain. (aspetjournals.org)
Accumulation1
- However, the observed reduction in endothelin-1 stimulated IP accumulation was still apparent in SHR when compared to WKY. (strath.ac.uk)
Cardiovascular1
- Endothelins have involvement in cardiovascular function, fluid-electrolyte homeostasis, and neuronal mechanisms across diverse cell types. (wikipedia.org)
Gene1
- Gender differences in genotypic distribution of endothelin-1 gene and endothelin receptor A gene in pulmonary hypertension associated with rheumatic mitral valve disease. (cdc.gov)
Roles1
- Mouse connective tissue mast cell proteases tryptase and carboxypeptidase A3 play protective roles in itch induced by endothelin-1. (iasp-pain.org)
Cell2
- The mouse mast cell proteases (mMCPs) mMCP4 (chymase), mMCP6 (tryptase), and CPA3 are found in connective tissue type mast cells and are the closest functional homologs to human mast cell proteases, but little is known about their role in endothelin-induced itch. (iasp-pain.org)
- Endothelin-1 produced a reduction in the extent of ADP-ribosylation of Gi alpha and this was of similar magnitude in both SHR and WKY cell membranes. (strath.ac.uk)