Genomes and Genes
Gene Symbol: Ednra
Description: endothelin receptor type A
Alias: ET-A, ET-AR, Endor, Eta, RGD1559432, endothelin-1 receptor, endothelin A receptor, endothelin-1 receptor-like
- Sugimoto K, Fujimori A, Yuyama H, Tahara A, Fujimura A. Renal protective effect of YM598, a selective endothelin type A receptor antagonist. J Cardiovasc Pharmacol. 2004;44 Suppl 1:S451-4 pubmed..These data suggest that endothelin is involved in the progression of diabetic nephropathy in OLETF rats, and an endothelin type A antagonist is promising for the treatment of diabetic nephropathy...
- Archer C, Robinson E, Drawnel F, Roderick H. Endothelin-1 promotes hypertrophic remodelling of cardiac myocytes by activating sustained signalling and transcription downstream of endothelin type A receptors. Cell Signal. 2017;36:240-254 pubmed publisher..These studies shed new light on strategies to pharmacologically intervene in the action of different pro-hypertrophic mediators. ..
- Lee J, Lee F, Huo T, Wang S, Huang H, Lin H, et al. Diabetes enhances the intrahepatic vascular response to endothelin-1 in cirrhotic rats: association with the ETA receptor and pERK up-regulation. Liver Int. 2015;35:704-12 pubmed publisher..The perfusion pressure changes in response to ET-1 were higher in the BDL/STZ group for all perfusates. ETA receptor and pERK expressions were enhanced in the BDL/STZ group...
- Kreipke C, Reynolds C, Schafer P, Schafer S, Pirooz R, Rafols J. Endothelin receptors A and B are expressed in distinct cellular compartments of rat hippocampus following global ischemia: an immunocytochemical study. Neurol Res. 2011;33:162-8 pubmed publisher..Additionally, endothelin receptor B increased expression in neurons and glia could be related to a more generalized activation of survival mechanisms involving elements of the neurovascular unit. ..
- Li P, Oparil S, Sun J, Thompson J, Chen Y. Fibroblast growth factor mediates hypoxia-induced endothelin-- a receptor expression in lung artery smooth muscle cells. J Appl Physiol (1985). 2003;95:643-51; discussion 863 pubmed
- Kwok C, Juan C, Shih K, Hwu C, Jap T, Ho L. Insulin-like growth factor-1 increases endothelin receptor A levels and action in cultured rat aortic smooth muscle cells. J Cell Biochem. 2005;94:1126-34 pubmed..These findings support the role of IGF-1 in the development of atherosclerotic, hypertensive, and diabetic vascular complications. ..
- Harris A, Elgebaly M, Li W, Sachidanandam K, Ergul A. Effect of chronic endothelin receptor antagonism on cerebrovascular function in type 2 diabetes. Am J Physiol Regul Integr Comp Physiol. 2008;294:R1213-9 pubmed publisher..dysfunction occurs in the Goto-Kakizaki (GK) model of Type 2 diabetes, and 2) pharmacological antagonism of ETA receptors ameliorates, while ETB receptor blockade augments vascular dysfunction...
- Afiatpour P, Latifpour J, Takahashi W, Yono M, Foster H, Ikeda K, et al. Developmental changes in the functional, biochemical and molecular properties of rat bladder endothelin receptors. Naunyn Schmiedebergs Arch Pharmacol. 2003;367:462-72 pubmed..This study indicates age-dependent alterations in the ET receptor system at both gene transcript and protein levels in the Fischer rat detrusor. ..
- Oktar B, Gülpinar M, Bozkurt A, Ghandour S, Cetinel S, Moini H, et al. Endothelin receptor blockers reduce I/R-induced intestinal mucosal injury: role of blood flow. Am J Physiol Gastrointest Liver Physiol. 2002;282:G647-55 pubmed..Furthermore, ET is involved in the pathogenesis of post-reperfusion-induced damage and beneficial effects of ET receptor antagonism are related to an improvement of disturbed blood flow during the reperfusion period...
- Sun L, Zhang W, Wang X, Song J, Li M. Inhibition of protein kinase C signal reduces ET receptor expression and basilar vasospasm after subarachnoid hemorrhage in rats. J Integr Neurosci. 2012;11:439-51 pubmed publisher..Application of RO-31-7549 reduced the expression of ET receptors and reduced cerebral vasospasm, suggesting that inhibition of PKC signaling pathway could effectively reduce DCVS after SAH. ..
- Piechota Polanczyk A, Kleniewska P, Goraca A. The influence of ETA and ETB receptor blockers on LPS-induced oxidative stress and NF-?B signaling pathway in heart. Gen Physiol Biophys. 2012;31:271-8 pubmed publisherThe aim of this study was to assess whether an endothelin-A receptor (ETA-R) blocker, BQ123, or an endothelin-B (ETB-R) receptor blocker, BQ788, influences nuclear factor kappa beta (NF-?B) pathway, free radical generation, tumor ..
- Sanchez A, Martinez P, Munoz M, Benedito S, Garcia Sacristan A, Hernandez M, et al. Endothelin-1 contributes to endothelial dysfunction and enhanced vasoconstriction through augmented superoxide production in penile arteries from insulin-resistant obese rats: role of ET(A) and ET(B) receptors. Br J Pharmacol. 2014;171:5682-95 pubmed publisher..Selective ETA (BQ123) or ETB receptor (BQ788) antagonists reduced both basal and ET-1-stimulated superoxide generation and ..
- Puppala B, Bhalla S, Matwyshyn G, Gulati A. Involvement of central endothelin receptors in neonatal morphine withdrawal. Exp Biol Med (Maywood). 2006;231:1157-60 pubmed..43%, EC50 = 13.26 nM) and morphine-withdrawal groups (75.08%, EC(50) = 11.70 nM), respectively. To our knowledge, this is the first report indicating involvement of central ET(A) receptors in neonatal morphine withdrawal. ..
- Lee T, Chen C, Lin M, Chang N. Effect of endothelin receptor antagonists on ventricular susceptibility in postinfarcted rats. Am J Physiol Heart Circ Physiol. 2008;294:H1871-9 pubmed publisher..Independent of their hemodynamic effects, a chronic use of either ET(A) or ET(A)/ET(B) antagonists may modify the arrhythmogenic response to programmed electrical stimulation. ..
- Bikhazi A, Khalifeh A, Jaroudi W, Saadeddine R, Jurjus A, El Sabban M, et al. Endothelin-1 receptor subtypes expression and binding in a perfused rat model of myocardial infarction. Comp Biochem Physiol C Toxicol Pharmacol. 2003;134:35-43 pubmed..These findings stipulate that during 1 month post-MI some biochemical and hormonal effects could alter ET-1 receptor subtype(s) regulation and pharmacodynamics thus predisposing to cardiac hypertrophy and mitogenesis. ..
- de Andrade C, Leite P, Montezano A, Casolari D, Yogi A, Tostes R, et al. Increased endothelin-1 reactivity and endothelial dysfunction in carotid arteries from rats with hyperhomocysteinemia. Br J Pharmacol. 2009;157:568-80 pubmed publisher..ET-1 activation of ET(A) receptors in HHcy changed the balance between endothelium-derived relaxing and contracting factors, favouring enhanced contractility. ..
- Liu M, Tian D, Wang T, Tang W, Liang K. Correlation between pulmonary endothelin receptors and alveolar-arterial oxygen gradient in rats with hepatopulmonary syndrome. J Huazhong Univ Sci Technolog Med Sci. 2005;25:494-6 pubmed..58 +/- 0.16 vs 0.28 +/- 0.07, P < 0.05). The expression of ETRB in lung was positively correlated with A-aDO2 (P < 0.05). It was concluded that the widened A-aDO2 may be related with enhancement of the expression of ETRB in lung. ..
- Sachidanandam K, Elgebaly M, Harris A, Hutchinson J, Mezzetti E, Portik Dobos V, et al. Effect of chronic and selective endothelin receptor antagonism on microvascular function in type 2 diabetes. Am J Physiol Heart Circ Physiol. 2008;294:H2743-9 pubmed publisher..Diabetic and control rats received an antagonist to either the ET type A (ETA; atrasentan; 5 mg x kg(-1) x day(-1)) or type B (ET(B); A-192621; 15 or 30 mg x kg(-1) x day(-1)) receptors for 4 ..
- Chies A, de Oliveira P, Rossignoli P, Baptista R, de Labio R, Payão S. Prostanoids counterbalance the synergism between endothelin-1 and angiotensin II in mesenteric veins of trained rats. Peptides. 2017;88:67-73 pubmed publisher..On the other hand, vasodilator prostanoids are mobilized to act in parallel with NO in order to counterbalance the Ang II responses that have been potentiated by ET-1 in these trained animals. ..
- Jain R, Shaul P, Borok Z, Willis B. Endothelin-1 induces alveolar epithelial-mesenchymal transition through endothelin type A receptor-mediated production of TGF-beta1. Am J Respir Cell Mol Biol. 2007;37:38-47 pubmed..These findings increase our basic understanding of the role of ET-1 in pulmonary fibrosis and suggest potential roles for AEC-derived ET-1 in the pathogenesis of other alveolar epithelial-mediated lung diseases. ..
- Richter M, Cloutier S, Sirois P. Endothelin, PAF and thromboxane A2 in allergic pulmonary hyperreactivity in mice. Prostaglandins Leukot Essent Fatty Acids. 2007;76:299-308 pubmed..These results suggest an important role for endothelin, PAF and thromboxane A2 in AHR in mice actively sensitized and challenged with ovalbumin. ..
- Yoon S, Zuccarello M, Rapoport R. EndothelinA-endothelinB receptor cross-talk in rat basilar artery in situ. Naunyn Schmiedebergs Arch Pharmacol. 2012;385:437-41 pubmed publisher..These findings suggest that the inability of ET(A) receptor antagonist to completely relax the ET-1 plateau contraction in rat basilar artery is due to ET(A)-ET(B) receptor cross-talk. ..
- Benjafield A, Katyk K, Morris B. Association of EDNRA, but not WNK4 or FKBP1B, polymorphisms with essential hypertension. Clin Genet. 2003;64:433-8 pubmed..These encoded the endothelin receptor type A (EDNRA), which transduces most of the vasoconstrictive properties of endothelin-1, protein kinase lysine deficient 4 (..
- Klinger F, Grimm R, Steinbach A, Tanneberger M, Kunert Keil C, Rettig R, et al. Low NaCl intake elevates renal medullary endothelin-1 and endothelin A (ETA) receptor mRNA but not the sensitivity of renal Na+ excretion to ETA receptor blockade in rats. Acta Physiol (Oxf). 2008;192:429-42 pubmed..Higher expression levels on low NaCl intake are AT(1) receptor dependent but are not associated with increased sensitivity of renal sodium handling to ET(A) receptor blockade. ..
- Jesmin S, Sakuma I, Togashi H, Yoshioka M, Hattori Y, Kitabatake A, et al. Effects of endothelin receptor antagonist on expression of AT1 and AT2 receptors in the heart of SHR-SP. J Cardiovasc Pharmacol. 2004;44 Suppl 1:S59-63 pubmed
- Kuwaki T, Ling G, Onodera M, Ishii T, Nakamura A, Ju K, et al. Endothelin in the central control of cardiovascular and respiratory functions. Clin Exp Pharmacol Physiol. 1999;26:989-94 pubmed..To address this question, we examined ABP and ventilation in mutant mice deficient in ET-1, ETA and ETB receptors and endothelin-converting enzyme-1, which were made by gene targeting. 2...
- Kendirci M, Pradhan L, Trost L, Gur S, Chandra S, Agrawal K, et al. Peripheral mechanisms of erectile dysfunction in a rat model of chronic cocaine use. Eur Urol. 2007;52:555-63 pubmed..The pathophysiologic mechanisms that are likely involved include increased plasma big-ET-1 levels, increased penile ET(A)R expression, increased penile MPO activity, and reduced penile eNOS expression. ..
- Fujimori A, Miyauchi T, Sakai S, Yuyama H, Iemitsu M, Sanagi M, et al. YM598, an orally active ET(A) receptor antagonist, ameliorates the progression of cardiopulmonary changes and both-side heart failure in rats with cor pulmonale and myocardial infarction. J Cardiovasc Pharmacol. 2004;44 Suppl 1:S354-7 pubmedThe effects of the novel, selective endothelin-A (ETA) receptor antagonist YM598 on both-side heart failure were investigated...
- Ge Y, Stricklett P, Hughes A, Yanagisawa M, Kohan D. Collecting duct-specific knockout of the endothelin A receptor alters renal vasopressin responsiveness, but not sodium excretion or blood pressure. Am J Physiol Renal Physiol. 2005;289:F692-8 pubmed..Furthermore, the CD ET(A) receptor does not appear to be involved in modulation of systemic blood pressure or renal Na excretion under physiological conditions. ..
- Usmani S, Appleton C, Beier F. Transforming growth factor-alpha induces endothelin receptor A expression in osteoarthritis. J Orthop Res. 2012;30:1391-7 pubmed publisher..Expression of ET(A)R protein and its encoding gene Ednra was assessed...
- Ikebe M, Nonoguchi H, Nakayama Y, Tashima Y, Shimada K, Tanzawa K, et al. Regulation of endothelin-converting enzyme 1 in nephrotic syndrome in rats. Nephron Exp Nephrol. 2003;94:e137-45 pubmed..The expression of prepro ET-1, ET-converting enzyme 1 (ECE-1), and ET A receptor mRNAs, but not ET B receptor mRNA, in the glomeruli was increased in rats with nephrotic syndrome...
- Talati M, West J, Blackwell T, Loyd J, Meyrick B. BMPR2 mutation alters the lung macrophage endothelin-1 cascade in a mouse model and patients with heritable pulmonary artery hypertension. Am J Physiol Lung Cell Mol Physiol. 2010;299:L363-73 pubmed publisher..This is the first description of protein expression that distinguishes HPAH from IPAH in patients. ..
- Yatawara A, Wilson J, Taylor L, Polgar P, Mierke D. C-terminus of ETA/ETB receptors regulate endothelin-1 signal transmission. J Pept Sci. 2013;19:257-62 pubmed publisherThe dimerization of the G protein-coupled receptors for endothelin-1 (ET-1), endothelin A receptor (ETA) and endolethin B receptor (ETB), is well established...
- Imamura T, Huang J, Dalle S, Ugi S, Usui I, Luttrell L, et al. beta -Arrestin-mediated recruitment of the Src family kinase Yes mediates endothelin-1-stimulated glucose transport. J Biol Chem. 2001;276:43663-7 pubmedThe insulin and the endothelin type A (ETA) receptor both can couple into the heterotrimeric G protein alpha(q/11) (Galpha(q/11)), leading to Galpha(q/11) tyrosine phosphorylation, phosphatidylinositol 3-kinase activation, and subsequent ..
- Legos J, Lenhard S, Haimbach R, Schaeffer T, Bentley R, McVey M, et al. SB 234551 selective ET(A) receptor antagonism: perfusion/diffusion MRI used to define treatable stroke model, time to treatment and mechanism of protection. Exp Neurol. 2008;212:53-62 pubmed publisher..In addition, tissue perfusion information obtained under these conditions might clarify mechanism of protection in the evaluation of protective compounds for focal stroke. ..
- Rodriguez M, Sabbatini M, Santella G, Vescina C, Vatta M, Bianciotti L. Vagally mediated cholestatic and choleretic effects of centrally applied Endothelin-1 through ETA receptors. Regul Pept. 2006;135:54-62 pubmed..the choleretic and the cholestatic effects of ET-1 were abolished in animals pretreated with icv BQ-610 (selective ETA antagonist) but not with BQ-788 (selective ETB antagonist)...
- Jesmin S, Sakuma I, Togashi H, Yoshioka M, Hattori Y, Kitabatake A, et al. Expression of endothelin receptors in the brain of SHR-SP and effects of an endothelin blocker. J Cardiovasc Pharmacol. 2004;44 Suppl 1:S156-9 pubmed
- Wagner M, Goltz D, Stucke C, Schwoerer A, Ehmke H, Volk T. Modulation of the transient outward K+ current by inhibition of endothelin-A receptors in normal and hypertrophied rat hearts. Pflugers Arch. 2007;454:595-604 pubmed
- Perry M, Molero M, Giulumian A, Katakam P, Pollock J, Pollock D, et al. ET(B) receptor-deficient rats exhibit reduced contraction to ET-1 despite an increase in ET(A) receptors. Am J Physiol Heart Circ Physiol. 2001;281:H2680-6 pubmed..Reduced contraction may be related to elevated plasma ET-1 and occurs in the presence of increased ET(A) receptor protein expression, suggesting an uncoupling of ET(A) receptor expression from functional activity...
- Johnström P, Fryer T, Richards H, Barret O, Clark J, Ohlstein E, et al. In vivo imaging of cardiovascular endothelin receptors using the novel radiolabelled antagonist [18F]-SB209670 and positron emission tomography (microPET). J Cardiovasc Pharmacol. 2004;44 Suppl 1:S34-8 pubmed..However, visualization of uptake in the rat heart was achievable and dynamic PET data together with the in vitro results suggest that [F]-SB209670 binds rapidly and primarily to endothelin-A receptors in the heart. ..
- Arrick D, Mayhan W. Inhibition of endothelin-1 receptors improves impaired nitric oxide synthase-dependent dilation of cerebral arterioles in type-1 diabetic rats. Microcirculation. 2010;17:439-46 pubmed publisher..We suggest that activation of ET(A) receptors during type-1 diabetes mellitus plays an important role in impaired eNOS- and nNOS-dependent dilation of cerebral arterioles. ..
- Compeer M, Suylen D, Hackeng T, De Mey J. Endothelin-1 and -2: two amino acids matter. Life Sci. 2012;91:607-12 pubmed publisher..This involves roles of amino acids on position 6 and 7 of the endothelin sequence. Agonist-dependent pathologies may benefit from the design of specific, agonist-selective ET-receptor antagonists. ..
- Francis B, Winaver J, Karram T, Hoffman A, Abassi Z. Renal and systemic effects of chronic blockade of ET(A) or ET(B) receptors in normal rats and animals with experimental heart failure. J Cardiovasc Pharmacol. 2004;44 Suppl 1:S54-8 pubmed
- Cheng Y, Dai D, Dai Y. Testis dysfunction by isoproterenol is mediated by upregulating endothelin receptor A, leptin and protein kinase Cvarepsilon and is attenuated by an endothelin receptor antagonist CPU0213. Reprod Toxicol. 2010;29:421-6 pubmed publisher..Over-expression of ET(A) and leptin accounting for the testis dysfunction is likely to be mediated by pPKCvarepsilon in the ISO treated rats. The upregulated ET pathway appears to be critical in pathologies of the testis...
- Gormley K, Bevan S, Hassan A, Markus H. Polymorphisms in genes of the endothelin system and cerebral small-vessel disease. Stroke. 2005;36:1656-60 pubmed..Polymorphisms in the ET-1 gene (K198N), the ET receptor type A (ETA), (-231G>A and +1222C>T), and the ET type B (ETB) receptor (G57S and L277L) were genotyped...
- Matsumoto T, Ishida K, Nakayama N, Kobayashi T, Kamata K. Involvement of NO and MEK/ERK pathway in enhancement of endothelin-1-induced mesenteric artery contraction in later-stage type 2 diabetic Goto-Kakizaki rat. Am J Physiol Heart Circ Physiol. 2009;296:H1388-97 pubmed publisher..These results suggest that upregulation of ET(A), a defect in ET(B)-mediated NO signaling, and activation of the MEK/ERK pathway together represent a likely mechanism mediating the hyperreactivity to ET-1 examined in this study. ..
- Chen G, Sun Z. Effects of chronic cold exposure on the endothelin system. J Appl Physiol (1985). 2006;100:1719-26 pubmed..We hypothesized that cold exposure increases ET-1 production and upregulates ET type A (ETA) receptors. The aim of this study was to determine the effect of cold exposure on regulation of the ET system...
- Ukai M, Yuyama H, Noguchi Y, Someya A, Okutsu H, Watanabe M, et al. Participation of endogenous endothelin and ETA receptor in premicturition contractions in rats with bladder outlet obstruction. Naunyn Schmiedebergs Arch Pharmacol. 2006;373:197-203 pubmed
- Konrad D, Haney M, Johansson G, Wanecek M, Weitzberg E, Oldner A. Cardiac effects of endothelin receptor antagonism in endotoxemic pigs. Am J Physiol Heart Circ Physiol. 2007;293:H988-96 pubmed..Positive hemodynamic effects from ET receptor antagonism in acute endotoxemia may be due to changes in cardiac load and enhanced diastolic function rather than improved contractile function. ..
- Johnson R, Fink G, Watts S, Galligan J. Endothelin receptor function in mesenteric veins from deoxycorticosterone acetate salt-hypertensive rats. J Hypertens. 2002;20:665-76 pubmed..Therefore, the sustained increase in venomotor tone mediated by ET(A) receptors that is known to occur in vivo in DOCA-salt hypertensive rats is not caused by direct venoconstriction. ..
- Chichorro J, Fiuza C, Bressan E, Claudino R, Leite D, Rae G. Endothelins as pronociceptive mediators of the rat trigeminal system: role of ETA and ETB receptors. Brain Res. 2010;1345:73-83 pubmed publisher..Taken together, these findings suggest that endothelins, acting through ET(A) and/or ET(B) receptors, may play an important role in mediating pain resulting from activation of most trigeminal nerve branches. ..