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EndothelinsReceptors, EndothelinReceptor, Endothelin AEndothelin-2Receptor, Endothelin BEndothelin-3Endothelin-1Viper VenomsPeptides, CyclicSulfonamidesAspartic Acid EndopeptidasesTachyphylaxisNeprilysinPyrrolidinesVasoconstrictor AgentsMetalloendopeptidasesVasoconstrictionPiperidinesOligopeptidesAdrenergic AgentsPhenylpropionatesGlycopeptidesEndothelium, VascularProtein PrecursorsPolymethacrylic AcidsRats, Sprague-DawleyPeptidesRats, WistarNitric OxideRNA, MessengerBlood PressureMuscle ContractionPeptide FragmentsKidneyThermolysinCells, CulturedMuscle, SmoothDose-Response Relationship, DrugBinding, CompetitiveMolecular Sequence DataAzepinesIndansAmino Acid SequenceProtein Kinase CChromatography, High Pressure LiquidKineticsAntihypertensive Agents
PeptidesExtracellularReceptorProteinsVasoactiveAortaNeuronsEndothelialHypertensionVascularMediatorsEffectsCellApproximatelyActivationSimilarCellsPeptidesVasoconstrictorPotentProstaglandinVitroIsopeptidesAbstractPrecursorPulmonary hypertensionConcentrationsInotropicGenePmolCurvesKIDNEYConcludeLevelsActivityUniquePatientsDepartmentOriginalHighActivitiesIsolated rat
Peptides3
  • 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)
  • These peptides are converted into inactive 38- or 39-amino acid intermediates called Big ETs (Big ET-1, Big ET-2, and Big ET-3) by furin-like endopeptidase. (encyclopedia.pub)
  • Endothelins are endothelium-derived vasoconstrictor peptides. (bestbiochem.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)
Receptor7
  • 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)
  • Within this research we looked into ET receptor expression in DRG and using the patch clamp technique the effects of ET-1 on responses to capsaicin in DRG neurons. (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)
  • In contrast to skeletal muscle resistance vessels, ET-1 contributes to the maintenance of skin microvascular tone through both ET A and ET B receptor-mediated vasoconstriction [ 16 ]. (biomedcentral.com)
  • The EDNRB gene provides instructions for making a protein called endothelin receptor type B. When this protein interacts with other proteins called endothelins, it transmits information from outside the cell to inside the cell, signaling for many important cellular processes. (medlineplus.gov)
  • The EDN3 gene provides instructions for a protein called endothelin 3, one of the endothelins that interacts with endothelin receptor type B. Together, endothelin 3 and endothelin receptor type B play an important role in the normal formation of enteric nerves. (medlineplus.gov)
  • Changes in either the EDNRB gene or the EDN3 gene disrupt the normal functioning of the endothelin receptor type B or the endothelin 3 protein, preventing them from transmitting signals important for the development of enteric nerves. (medlineplus.gov)
Proteins1
  • 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)
Vasoactive3
  • 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)
  • The present study aimed to investigate the involvement of the vasoactive substances ET-1 and nitric oxide (NO) in intermediate/cold type CRPS1 in relation to inflammatory mediators. (biomedcentral.com)
  • 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)
Aorta1
  • 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)
Neurons4
  • ET-1 highly potentiated capsaicin-induced TRPV1 currents in a few neurons and in HEK293 cells co-expressing TRPV1 as well as the ETAR. (exposed-skin-care.net)
  • Given the amount of reports in the participation of ET-1 in nociception fairly little is well known about the signaling cascade and effectors that result in the nociceptive replies to ET-1 in principal sensory neurons. (exposed-skin-care.net)
  • A subpopulation of neurons responded to ET-1 with a potentiation of the capsaicin-mediated responses. (exposed-skin-care.net)
  • In addition to ECs, ET-1 is expressed in a wide variety of cells including VSMCs, cardiomyocytes, fibroblasts, macrophages, epithelial cells in the lungs and kidneys, neurons, and glial cells [ 13 ] . (encyclopedia.pub)
Endothelial3
  • In HTN, the delicate balance between vasodilators and vasoconstrictors is disturbed, leading to endothelial dysfunction (ED) with excessive release of vasoconstrictor substances, such as ET-1 [ 9 ] [ 10 ] . (encyclopedia.pub)
  • ET-1 was first isolated in 1988 by Yanagisawa and colleagues from the culture supernatant of porcine aortic endothelial cells (ECs). (encyclopedia.pub)
  • Schematic representation of the biosynthesis and vascular effects of ET-1 in endothelial and smooth muscle cells. (encyclopedia.pub)
Hypertension2
  • Endothelin-1 and Hypertension" Encyclopedia , https://encyclopedia.pub/entry/14671 (accessed November 30, 2023). (encyclopedia.pub)
  • Hypertension (HTN) is one of the most prevalent socially significant diseases and is among the most important preventable risk factors for other diseases [ 1 ] . (encyclopedia.pub)
Vascular2
  • In complex regional pain syndrome type 1 (CRPS1) pro-inflammatory mediators and vascular changes play an important role in the sustained development and outcome of the disease. (biomedcentral.com)
  • ET-1 is the predominant isopeptide involved in regulating the cardiovascular system, and vascular ECs are the most abundant source of ET-1. (encyclopedia.pub)
Mediators1
  • 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)
Effects3
  • To investigate the signaling pathways involved in potentiation we analyzed the effects of ET-1 in HEK293 cells coexpressing the ETAR and TRPV1. (exposed-skin-care.net)
  • 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)
  • Endothelins have been reported to exert a wide range of electrophysiological effects in mammalian cardiac cells. (mtak.hu)
Cell1
  • 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)
Approximately2
  • The endothelins (ETs) are produced from their corresponding approximately 200-residue prepropolypeptides that are encoded by three distinct genes. (encyclopedia.pub)
  • Hirschsprung disease occurs in approximately 1 in 5,000 newborns. (medlineplus.gov)
Activation1
  • The voltage dependence of steady-state activation and inactivation was not altered by ET-1. (mtak.hu)
Similar1
  • Shortly after the discovery of ET-1, two other structurally similar isopeptides, named ET-2 and ET-3, were isolated [ 12 ] . (encyclopedia.pub)
Cells1
  • Endothelin-1 (10(-6) M) stimulated IP formation was decreased in cells from SHR compared to WKY (WKY 1117 +/- 157, SHR 668 +/- 85% of basal). (strath.ac.uk)
Peptides2
Vasoconstrictor5
  • Endothelin-1 (ET-1), a potent vasoconstrictor peptide produced by endothelial cells and degraded predominantly in the pulmonary vasculature, has been implicated in the development of various organ dysfunctions. (nih.gov)
  • We examined the effects of the vasoconstrictor peptide endothelin-1 in the isolated heart and defined interactions of endothelin-1 with other hormone systems. (ox.ac.uk)
  • The effect of high dosages (40 and 400 pmol) of endothelin-1 on coronary flow was biphasic, with an early vasodilator and a late vasoconstrictor component that was irreversible. (ox.ac.uk)
  • Putative precursors of endothelin have less vasoconstrictor activity in vitro but a potent pressor effect in vivo. (jamanetwork.com)
  • Cloning and sequence analysis of cDNA encoding the precursor of a human endothelin-derived vasoconstrictor peptide, endothelin: identity of human and porcine endothelin. (jamanetwork.com)
Potent1
  • Gandhi CRStephenson KOlson MS Endothelin, a potent peptide agonist in the liver. (jamanetwork.com)
Prostaglandin2
  • Neither alpha- nor beta-blocking agents (phentolamine and propranolol) nor the Ca2(+)-channel blocker nifedipine altered the effects of endothelin-1, but prostaglandin synthesis inhibition by indomethacin significantly augmented vasoconstriction by endothelin-1. (ox.ac.uk)
  • McMillen MHuribal MKumar RSumpio BE Endothelin-stimulated human monocytes produce prostaglandin E2 but not leukotriene B4. (jamanetwork.com)
Vitro1
Isopeptides1
  • The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes. (jamanetwork.com)
Abstract2
  • Watanabe TXKumagaya SNishio HNakajima KKimura TSakakibara S Effects of endothelin-1 and endothelin-3 on blood pressure in conscious hypertensive rats [abstract]. (jamanetwork.com)
  • abstract = "RES-701-1 (cyclic (Gly1Asp9)(GlyAsnTrpHisGlyThrAlaProAspTrp PhePheAsnTyrTyrTrp)), a peptide isolated from Streptomyces sp. (unair.ac.id)
Precursor1
Pulmonary hypertension2
  • To obtain comparable conditions in both groups, the ET-1 level was raised in the control group by exogenous infusion (0.4 pmol/kg/min) to 9.4 +/- 0.8 pmol/L. ARDS was accompanied by a hyperdynamic circulatory pattern with increased cardiac output and depressed total vascular resistance but, simultaneously, pulmonary hypertension. (nih.gov)
  • Circulating immunoreactive endothelin-1 in children with pulmonary hypertension. (jamanetwork.com)
Concentrations3
  • We conclude that ET-1 concentrations are elevated in ARDS as the result of both increased formation and decreased disposal. (nih.gov)
  • Endothelin-3 has been found in high concentrations in the brain and may regulate important functions in neurons and astrocytes, such as proliferation and development. (lookformedical.com)
  • Elevated plasma endothelin-1 concentrations are associated with the severity of illness in patients with sepsis. (jamanetwork.com)
Inotropic2
  • Endothelin-1 (ET-1) is known with its direct positive inotropic and chronotropic effects on isolated heart and with growth effects. (nih.gov)
  • Vigne PLazdunski MFrelin C The inotropic effect of endothelin-1 on rat atria involves hydrolysis of phosphatidylinositol. (jamanetwork.com)
Gene2
  • The aim of this pilot study was to investigate the frequency distribution of the common polymorphism of the ET-1 gene and its possible relation with hemodynamic consequences of malignant ventricular arrhythmias in patients with structural heart disease. (nih.gov)
  • Bloch KDEddy RLShows TBQuertermous T cDNA cloning and chromosomal assignment of the gene encoding endothelin 3. (jamanetwork.com)
Pmol4
  • In control subjects, the lung cleared the major fraction of ET-1 (fractional extraction 43 +/- 8.8%, uptake 12.5 +/- 2.5 pmol/min). (nih.gov)
  • First, the effect of a single bolus of endothelin-1 (4-400 pmol) was followed for 90 min. (ox.ac.uk)
  • Second, cumulative dose-response curves were obtained for endothelin-1 boluses of 0.04-400 pmol. (ox.ac.uk)
  • Angiotensin-converting enzyme (ACE) inhibition by captopril antagonized endothelin-1-dependent vasoconstriction to a small extent at 400 pmol. (ox.ac.uk)
Curves1
  • In the aorta with endothelium, 3 μM RES-701-1 shifted the concentration-response curves for the contractile effects of endothelin-1 and endothelin-3 to the left. (unair.ac.id)
KIDNEY1
Conclude1
  • We conclude that in isolated rat heart endothelin-1 causes marked and long-lasting coronary constriction. (ox.ac.uk)
Levels4
  • To determine the pathophysiologic role of ET-1 in adult respiratory distress syndrome (ARDS) and the impact of impaired lung function on transpulmonary peptide handling, we compared plasma levels and pulmonary ET-1 balance in 14 patients with ARDS and in seven healthy control subjects. (nih.gov)
  • It may play a role in reducing systemic ENDOTHELIN levels. (lookformedical.com)
  • Increased plasma levels of endothelin-1 and big endothelin-1 in acute myocardial infarction [letter]. (jamanetwork.com)
  • Endothelin-1, interleukin-6, and interleukin-8 levels increase in patients with burns. (jamanetwork.com)
Activity1
Unique1
Patients1
  • Plasma immunoreactive endothelin in the acute and subacute phases of myocardial infarction in patients undergoing fibrinolysis. (jamanetwork.com)
Department1
  • 1 Department of Medicine III, Vienna Medical School, Austria. (nih.gov)
Original1
  • Taq polymorphism of ET-1 was detected using our original polymerase chain reaction method. (nih.gov)
High2
Activities1
  • Le JVilcek J Tumor necrosis factor and interleukin 1: cytokines with multiple overlapping biological activities. (jamanetwork.com)
Isolated rat1
  • In isolated rat aorta without endothelium, 10 μM RES-701-1 did not affect the resting tone, nor did it attenuate the contractions induced by endothelin-1, endothelin-3 or norepinephrine. (unair.ac.id)