There are no specific protocols for Recombinant Human Endothelin B Receptor protein (ab114259). Please download our general protocols booklet
TY - JOUR. T1 - Endothelin B receptor deficiency potentiates ET-1 and hypoxic pulmonary vasoconstriction. AU - Ivy, D. Dunbar. AU - Mcmurtry, Ivan F.. AU - Yanagisawa, Masashi. AU - Gariepy, Cheryl E.. AU - Le Cras, Timothy D.. AU - Gebb, Sarah A.. AU - Morris, Kenneth G.. AU - Wiseman, Richard C.. AU - Abman, Steven H.. PY - 2001/5. Y1 - 2001/5. N2 - Endothelin (ET)-1 contributes to the regulation of pulmonary vascular tone by stimulation of the ETA and ETB receptors. Although activation of the ETA receptor causes vasoconstriction, stimulation of the ETB receptors can elicit either vasodilation or vasoconstriction. To examine the physiological role of the ETB receptor in the pulmonary circulation, we studied a genetic rat model of ETB receptor deficiency [transgenic(sl/sl)]. We hypothesized that deficiency of the ETB receptor would predispose the transgenic(sl/sl) rat lung circulation to enhanced pulmonary vasoconstriction. We found that the lungs of transgenic(sl/sl) rats are ETB deficient ...
Alterations in the methylation patterns of promoter CpG islands have been associated with the transcriptional inhibition of genes in many human cancers. These epigenetic alterations could be used as molecular markers for the early detection of cancer-that is, while potentially curable according to current therapeutic strategies. In prostate cancer, GSTP1 hypermethylation is the most common epigenetic alteration, and can be detected in up to 90% of cases. Thus, screening for methylation of other loci would probably increase the number of primary tumours amenable to screening. Moreover, previous studies have shown that the endothelin B receptor (EDNRB) gene is abnormally methylated in a high proportion of prostate tumours ( approximately 70%).. To investigate the potential use of EDNRB gene hypermethylation as a prostate cancer specific marker.. Methylation specific polymerase chain reaction (MSP) for the promoter region of EDNRB was performed on prospectively collected tissue samples from 48 ...
A highly selective peptide agonist of the endothelin-B receptor. Endothelin B receptor agonist SPI-1620 binds to endothelin-B receptors on endothelial cells in tumor blood vessels, which, unlike the angioarchitecture of normal blood vessels, are relatively devoid of smooth muscle. This agent may induce a transient, selective increase in blood flow to a tumor, which may result in an increase in the delivery of anticancer agents to the tumor and, so, an increase in anticancer agent efficacy.. ...
BioAssay record AID 66868 submitted by ChEMBL: Inhibition of (125 I)-endothelin 1 binding to endothelin B receptor in rat cerebellum.
TY - JOUR. T1 - Cyclosporine A-induced increase in glomerular cyclic GMP in rats and the involvement of the endothelin(B) receptor. AU - Tack, Ivan. AU - Marin-Castano, Encarna. AU - Bascands, Jean Loup. AU - Pecher, Christiane. AU - Ader, Jean Louis. AU - Girolami, Jean Pierre. PY - 1997. Y1 - 1997. N2 - 1. A transient two fold increase in the cyclic GMP content was observed in rat freshly isolated glomeruli 6 to 9 h after a single subcutaneous injection of 20 mg kg-1 cyclosporine A (CsA) in conscious animals. 2. In vitro stimulation with endothelin 3 (ET-3) of isolated glomeruli obtained from CsA-untreated rats resulted in a dose-dependent increase in cyclic GMP content. The increase observed with 10 nM ET-3 was similar to that observed in glomeruli isolated 9 h after in vivo CsA administration. 3. The rise in glomerular cyclic GMP content after in vivo CsA injection was prevented by in vivo treatment with L-NAME (10 mg kg-1) or by in vitro calcium deprivation of the incubation medium. 4. The ...
LifeSpan BioSciences currently sells 33 antibodies , 5 peptides , 11 ELISA Kits , 4 proteins specific for EDNRB / Endothelin B Receptor.
Buy our Endothelin B Receptor peptide. Ab109654 is a blocking peptide for ab95911 and has been validated in BL. Abcam provides free protocols, tips and expert…
Endothelin B Receptor Polyclonal Antibody from Invitrogen for Western Blot and Immunohistochemistry (Paraffin) applications. This antibody reacts with Human, Mouse, Rat samples. Supplied as 100 µL purified antibody (1 mg/ml) in PBS with 50% glycerol and 0.01% thimerosal; pH 7.
The potent vasoconstrictor endothelin-1 (ET-1) is at its highest concentration in the normal human ejaculate and is associated with the progression of metastatic prostate cancer. ET-1 protein expression is detected in situ in 14 of 14 primary cancers and 14 of 16 metastatic sites of human prostatic carcinoma. Exogenous ET-1 induces prostate cancer proliferation directly and enhances the mitogenic effects of insulin-like growth factor I, insulin-like growth factor II, platelet-derived growth factor, basic fibroblast growth factor, and epidermal growth factor in serum-free conditions in vitro. The ETA-selective receptor antagonist A-127722 inhibits ET-1-stimulated growth, but the ETB-selective receptor antagonist BQ-788 does not. ET-3, an ETB-selective agonist, also had no effect on prostate cancer growth. No specific ETB-binding sites could be demonstrated in any established human prostate cancer cell line tested, and ETB mRNA, detected by reverse transcription PCR, was reduced. The predominance ...
About one third of patients with type 1 diabetes develops kidney disease. The mechanism is largely unknown, but intrarenal hypoxia has been proposed as a unifying mechanism for chronic kidney disease including diabetic nephropathy. The endothelin system has recently been demonstrated to regulate oxygen availability in the diabetic kidney via a pathway involving endothelin type A receptors (ETA-R). These receptors mainly mediate vasoconstriction and tubular sodium retention, and inhibition of ETA-R improves intrarenal oxygenation in the diabetic kidney. Endothelin type B receptors (ETB-R) can induce vasodilation of the renal vasculature and also regulate tubular sodium handling. However, the role of ETB-R in kidney oxygen homeostasis is unknown. The effects of acute intrarenal ETB-R activation (Sarafotoxin 6c for 30-40 min; 0.78 pmol h-1 directly into the renal artery) on kidney function and oxygen metabolism were investigated in normoglycemic controls and insulinopenic male Sprague Dawley rats ...
About one third of patients with type 1 diabetes develops kidney disease. The mechanism is largely unknown, but intrarenal hypoxia has been proposed as a unifying mechanism for chronic kidney disease including diabetic nephropathy. The endothelin system has recently been demonstrated to regulate oxygen availability in the diabetic kidney via a pathway involving endothelin type A receptors (ETA-R). These receptors mainly mediate vasoconstriction and tubular sodium retention, and inhibition of ETA-R improves intrarenal oxygenation in the diabetic kidney. Endothelin type B receptors (ETB-R) can induce vasodilation of the renal vasculature and also regulate tubular sodium handling. However, the role of ETB-R in kidney oxygen homeostasis is unknown. The effects of acute intrarenal ETB-R activation (Sarafotoxin 6c for 30-40 min; 0.78 pmol h-1 directly into the renal artery) on kidney function and oxygen metabolism were investigated in normoglycemic controls and insulinopenic male Sprague Dawley rats ...
misc{9ad9b9f4-306e-41a1-8e16-4835068ccfb9, author = {Zheng, J and Zhang, Y and Edvinsson, Lars and Xu, C. -B}, issn = {1473-5598}, language = {eng}, note = {Conference Abstract}, number = {Suppl. 1}, pages = {24--24}, publisher = {Lippincott Williams & Wilkins}, series = {Journal of Hypertension}, title = {Vascular endothelin type B receptor upregulation correlates with activation of inflammatory transcriptional factor NF-kappaB}, volume = {26}, year = {2008 ...
article{b53dd734-d576-42ed-8e0f-a70425b980ab, abstract = {The aim of this study was to examine if endothelin ETB receptor-mediated contraction occurred in isolated segments of rat coronary arteries during organ culture. Presence of contractile endothelin ETB receptors was studied by measuring the change in isometric tension in rings of left anterior descending coronary arteries isolated from hearts of rats as response to application of the selective endothelin ETB receptor agonist, Sarafotoxin 6c and endothelin-1. In segments cultured 1 day in serum free Dulbeccos Modified Eagles Medium, Sarafotoxin 6c induced a concentration dependent contraction with pEC(50) value of 10.4 +/- 0.21 and a maximal response of 3.9 +/- 0.25 mN/mm (n = 15). The maximal contraction was significantly larger than the responses measured in fresh tissue, where the mean value of the maximal contractions was 0.22 +/- 0.03 mN/mm (n = 17). The increased contraction to Sarafotoxin 6c, after culturing could be eliminated ...
The vascular effects of the endothelin B (ETB) receptor agonist IRL 1620 were investigated in the rat P22 carcinosarcoma and a range of normal tissues in BDIX rats. Tissue blood flow rate was calculated from measurements of tissue uptake of radiolabelled iodoantipyrine. A comparison of vascular effects in the P22 tumour and the HSN sarcoma growing in CBH/CBi rats was made using laser Doppler flowmetry, showing similar effects of IRL 1620, with red cell flux rapidly decreasing by 50-60% and then returning to control levels within approximately 30 min. This corresponded to similar levels but different spatial organisation of ETB binding sites in the two tumours, as measured by autoradiography. The decrease in tumour blood flow and an increase in vascular resistance suggest that the vascular component of ETB receptors in the P22 tumour is localised on contractile elements rather than on endothelial cells. ETA receptors were also identified. Vasoconstriction occurred uniformly throughout the P22 ...
The region of the EDNRB gene promotor analysed in our study was chosen because of a previous study indicating that the most 3′ CpG dinucleotide was more heavily methylated than the 5′ end.30 Our results confirm this finding concerning the methylation status of adenocarcinoma samples. However, because of the high sensitivity (1/1000) of the MSP method used in our present study,36 we were also able to detect DNA hypermethylation in paired normal tissue and hyperplastic tissue from the control group (BPH). Moreover, the increased sensitivity of the method may explain the larger proportion of methylated tumours found in our present study. These findings are consistent with the results reported by Pao et al, who found that EDNRB methylation levels varied from 11% to 25% in all the five normal samples analysed, and varying from 11% to , 50% in the paired prostate tumours.35 Indeed, the primer sets used in our study included two CpG sites (−130 and −8) analysed in the aforementioned report.35 ...
TY - JOUR. T1 - Renal vasoconstriction to endothelin-1 is enhanced with blockade of endothelin-B receptors or nitric oxide production. AU - Stacy, D. L.. AU - Martinez, R.. AU - Tilton, Ronald. PY - 1996. Y1 - 1996. N2 - Endothelin (ET-1) is a potent renal vasoconstrictor causing an initial transient vasodilation due to activation of ETB receptors and a long-lasting vasoconstriction thought to be due to ETA and ETB receptors. In anesthetized rats ET-1 was infused intravenously {i.V., 1 nmole/kg) after BQ-123 (an ETA receptor antagonist), BQ-788 (an ETB receptor antagonist), or vehicle. Left renal artery flow and mean arterial pressure (MAP) were measured. Resistance was calculated as MAP/flow. ET-1 increased renal resistance by 248% (26±2 to 90±13 mmHg/ml/min.). After pretreatment with BQ-123 (1 mg/kg, i.V.), the increase in renal resistance with ET-1 was reduced by 77% (29±5 to 43±7 mmHg/ml/min.), due to a reduction in the increase in MAP by 81% and decrease in flow by 61%. Pretreatment ...
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Endothelins (ET-1, 2, and 3) are considered to be very powerful vasoconstrictive substances. In humans, endothelins mediate their actions via two…
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Microvascular dysfunction originating during a preeclamptic pregnancy persists postpartum and probably contributes to increased CVD risk in these women. One putative mechanism contributing to this dysfunction is increased vasoconstrictor sensitivity to endothelin-1 (ET-1), mediated by alterations in ET-1 receptor type-B (ETBR). We evaluated ET-1 sensitivity, ETAR, and ETBR contributions to ET-1-mediated constriction, and the mechanistic role of ETBR in endothelium-dependent dilation in vivo in the microvasculature of postpartum women who had preeclampsia (PrEC, n=12) and control women who had a healthy pregnancy (HC, n=12). We hypothesized that (1) PrEC would have a greater vasoconstrictor response to ET-1, and (2) reduced ETBR-mediated dilation. We further hypothesized that ETBR-blockade would attenuate endothelium-dependent vasodilation in HC, but not PrEC. Microvascular reactivity was assessed by measurement of cutaneous vascular conductance responses to graded infusion of ET-1 ...
Recent gene targeting studies have revealed unexpected roles for endothelins in the development of neural crest-derived tissues. Endothelin converting enzyme-1 (ECE-1) catalyzes the proteolytic activation of big endothelin-1 to endothelin-1(ET-1) in vitro. However, the importance of ECE-1 cleavage in the multiple endothelin pathways in vivo is unknown. Here we generated a targeted null mutation in the mouse ECE-1 gene. ECE-1−/− term embryos exhibited craniofacial and cardiac abnormalities virtually identical to the defects seen in ET-1 and endothelin A receptor (ETA)-deficient embryos. Epidermal melanocytes as well as enteric neurons of the distal gut were also absent in ECE-1−/− embryos, reproducing the developmental phenotype seen in ET-3−/− and endothelin B receptor (ETB)−/− mice. Surprisingly, large amounts of mature ET-1 peptide are found in ECE-1−/− embryos, indicating that non-ECE-1 protease(s) can activate ET-1 at certain sites. However, these enzymes cannot produce ...
EDNRB - EDNRB (Myc-DDK-tagged)-Human endothelin receptor type B (EDNRB), transcript variant 3 available for purchase from OriGene - Your Gene Company.
When Yanagisawa et al.1 first identified endothelin (ET), a novel polypeptide vasoconstrictor for which numerous other functions were identified later,2 there was early widespread enthusiasm and great expectation for therapeutic opportunities. ET-1 is the most powerful vasoconstrictor in this peptide family; the ET system is complex with a converting enzyme and two receptors, ETA-R and ETB-R. The receptors offer an opportunity for selective blockade. ETA-R primarily mediates vasoconstriction and plays a role in the genesis of hypertension, states of endothelial dysfunction, insulin resistance, inflammation, and fibrosis. From a renal perspective, it is important to note that both ETA-R and ETB-R are found in the kidney, ETA-R in vessels and ETB-R mainly in the medulla3 but also in glomeruli.4 Of note, collecting duct ETB-R null mice develop elevated BP, pointing to a potential causal role in the genesis of hypertension.5 It was immediately perceived that such a multifunctional system might ...
Activation of the endothelin A receptor (ET(A)) by endothelin-1 (ET-1) mediates events that regulate mitogenesis, apoptosis, angiogenesis and metastasis in tumours. Specific blockade of ET(A) may have anticancer effects, while retaining beneficial endothelin B receptor (ET(B))-mediated effects such …
Ednrb - Ednrb (untagged ORF) - Rat endothelin receptor type B (Ednrb), (10 ug) available for purchase from OriGene - Your Gene Company.
The investigational drug DEDN6526A, which is a new member of a class of drugs called antibody-drug conjugates, was safe, tolerable, and showed hints of activity against different forms of melanoma-cutaneous, mucosal, and ocular-according to results of a first-in-human phase I clinical trial presented here at the AACR Annual Meeting 2014, April 5-9.. Antibody-drug conjugates consist of an antibody attached to a toxic chemotherapy by a special linker that keeps the chemotherapy inactive. In the case of DEDN6526A, the antibody recognizes the protein endothelin B receptor (ETBR) and the toxic chemotherapy is monomethyl auristatin (MMAE). Infante explained that when administered to the patient, the antibody portion of DEDN6526A recognizes and attaches to ETBR, which is often present at elevated levels on the surface of tumor cells in patients with melanoma. The whole antibody-drug conjugate is then taken up by the cells and MMAE is released from the linker to become active, killing the melanoma ...
Selective endothelin A (ETA) and combined ETA and ETB receptor antagonists are being investigated for use in treating diabetic nephropathy. However, the receptor-specific mechanisms responsible for producing the potential benefits have not been discerned. Thus, we determined the actions of ETA and ETB receptors on measures of glomerular function and renal inflammation in the early stages of diabetic renal injury in rats through the use of selective and combined antagonists. Six weeks after streptozotocin (STZ)-induced hyperglycemia, rats were given 2R-(4-methoxyphenyl)-4S-(1,3-benzodioxol-5-yl)-1-(N,N-di(n-butyl)aminocarbonyl-methyl)-pyrrolidine-3R-carboxylic acid (ABT-627) (5 mg/kg/day), a selective ETA antagonist; (2R,3R,4S)-4-(benzo[d][1,3]dioxol-5-yl)-2-(3-fluoro-4-methoxyphenyl)-1-(2-(N-propylpentylsulfonamido)ethyl)pyrrolidine-3-carboxylic acid hydrochloride (A-182086) (10 mg/kg/day), a combined ETA/B antagonist; or vehicle for 1 week. Sham controls received STZ vehicle (saline). ...
mice on diet-induced hyperinsulinemia and hyperglycemia. The mechanism of insulins enhanced antiatherogenic actions in EC was related to remarkable induction of NO action, which increases endothelin receptor B (EDNRB) expression and intracellular [Ca2+]. Using the mice with knockin mutation of eNOS, which had Ser1176 mutated to alanine (AKI), deleting the only known mechanism for insulin to activate eNOS/NO pathway, we observed that IRS1 overexpression in the endothelia of ...
Affiliation:福岡大,医学部,講師, Research Field:Circulatory organs internal medicine,Circulatory organs internal medicine, Keywords:心房細動,ACE,dpGapoE,遺伝子多型,atrial fibrillation,candesartan,アンジオテンシン,スタチン,Endothelin type B receptor,再灌流, # of Research Projects:8, # of Research Products:11
Stable recombinant cell line expressing the Endothelin, ETB receptor. Human recombinant, in CHO-K1 host cell. We provide: Two vials of the recombinant cell line as frozen cells; Detailed product information including sequence, cell line properties, culture conditions, pharmacological properties of the recombinant receptor in binding and functional assays (cAMP). In addition, for total reassurance, we will provide up to two free replacements within in a 2 year period should you accidently lose your cell line ...
PURPOSE and BACKGROUND Cancers cells grow without the vices of responses control systems, leading to increased tumor cell success. platelets, tumor cells up-regulated down-regulated and anti-apoptotic pro-apoptotic genetics, elevated the amount of cells in the activity of DNA and reduced the accurate amount in the quiescent stage, elevated phrase of cyclins, DNA fix MAPKs and …Read More. ...
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Although the pulsatility (±1 mm Hg) and rate of perfusate flow (1 mL/min) through the isolated segments do not precisely match the conditions in the rabbit jugular vein in vivo, the newly developed model allowed us to study the effects of an enhanced perfusion pressure on gene expression in the vessel wall in situ. With the aid of this model, we were able to substantiate earlier findings in cultured endothelial cells of a stretch- and/or deformation-induced increase in prepro-ET-1 mRNA abundance9 and ET-1 release.7 8 The pressure-induced upregulation of prepro-ET-1 expression in the endothelium and that of the ETB-R in the smooth muscle did not follow the pattern of an all-or-nothing response but were clearly dependent on the duration and intensity of the increase in perfusion pressure. Most important, however, these changes in gene expression did not occur at physiological pressure levels that, depending on the animals posture and heart cycle, can be estimated for the external rabbit jugular ...
TY - JOUR. T1 - Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method. AU - Han, Seong Gu. AU - Ko, Sanghwan. AU - Lee, Won Kyu. AU - Jung, Sang Taek. AU - Yu, Yeon Gyu. PY - 2017/12/1. Y1 - 2017/12/1. N2 - G-protein coupled receptors (GPCRs) play indispensable physiological roles in cell proliferation, differentiation, and migration; therefore, identifying the mechanisms by which ligands bind to GPCRs is crucial for developing GPCR-targeting pharmaceutics and for understanding critical biological functions. Although some structural information is available regarding the interactions between GPCRs and their small molecule ligands, knowledge of how GPCRs interact with their corresponding macromolecule ligands, such as peptides and proteins, remains elusive. In this study, we have developed a novel strategy to investigate the precise ligand recognition mechanisms involved in the interaction of endothelin receptor type A (ETA) with its ...
The purpose of our study was to examine if lipopolysaccharide (LPS) from Porphyromonas gingivalis (P.g.) modifies the vasomotor responses to Endothelin-1 (ET-1) and Sarafotoxin 6c (S6c) in rat coronary arteries. The arteries were studied directly or following organ culture for 24 h in absence and presence of 2.5EU/ml LPS. The contractile responses of coronary arteries were investigated by using the selective ETB receptor agonist S6c (1 pM-0.3 μM) and ET-1 (1 pM-0.3 μM). The functional studies demonstrated an augmented contractile response only to S6c in isolated rat coronary arteries after organ culture (with or without LPS). These contractile responses by S6c were blocked by the selective ETB receptor antagonist BQ788 in both vessel groups. The augmented contractile response to S6c was supported by immunohistochemistry, where a significant increase in fluorescence intensity for ETB receptors in smooth muscle cells was observed after organ culture. The presence of LPS in the culture medium ...
In cardiovascular diseases, endothelin type B (ET(B)) receptors in arterial smooth muscle cells are upregulated. The present study revealed that organ culture of rat mesenteric artery segments enhanced endothelin ET(B) receptor-mediated contraction paralleled with increase in the receptor mRNA and protein expressions. The endothelin ET(B) receptor-mediated contraction was associated with increase in phosphorylation of extracellular regulation kinase 1 and 2 (ERK1/2) proteins and elevated levels of intracellular calcium. The elevation curve of intracellular calcium consisted of two phases: one rapid and one sustained. Inhibition of ERK1/2 phosphorylation by SB386023 or blockage of calcium channels by nifedipine significantly reduced the endothelin ET(B) receptor-mediated contraction (P,0.05) and decreased the sustained phase of intracellular calcium level, but not the rapid phase. Thus, phosphorylation of ERK1/2 proteins and elevation of intracellular calcium level are required for endothelin ...
Endothelin-1 (ET-1) is a neuroactive peptide produced by neurons, reactive astrocytes, and endothelial cells in the brain. Elevated levels of ET-1 have been detected in the post-mortem brains of individuals with Alzheimers disease (AD). We have previously demonstrated that overexpression of astrocytic ET-1 exacerbates memory deficits in aged mice or in APPK670/M671 mutant mice. However, the effects of ET-1 on neuronal dysfunction remain elusive. ET-1 has been reported to mediate superoxide formation in the vascular system via NADPH oxidase (NOX) and to regulate the actin cytoskeleton of cancer cell lines via the cofilin pathway. Interestingly, oxidative stress and cofilin activation were both reported to mediate one of the AD histopathologies, cofilin rod formation in neurons. This raises the possibility that ET-1 mediates neurodegeneration via oxidative stress- or cofilin activation-driven cofilin rod formation. Here, we demonstrate that exposure to 100 nM ET-1 or to a selective ET type B ...
Left: The EDNRB gene may play a role in Ethiopians adaptation to life at high altitudes. Right: EDNRB coordinates a network of genes involved in heart function.. Ethiopians have lived at high altitudes for thousands of years, providing a natural experiment for studying human adaptations to low oxygen, a condition known as hypoxia. One factor that may enable Ethiopians to tolerate high altitudes and hypoxia is the endothelin receptor type B (EDNRB) gene. Researchers at University of California, San Diego School of Medicine now find that mice with lower-than-normal levels of EDNRB protein are remarkably tolerant to hypoxia. The study, published this week by the Proceedings of the National Academy of Sciences, provides a mechanism for the genes role in adaptation to life at high altitudes and suggests that EDNRB could be targeted to treat sea level diseases that stem from lack of oxygen.. This is the first demonstration that a gene involved in high altitude adaptation is critical in protecting ...
Endothelin-1 (ET-1) is a potent mitogen and modulator of vascular tone. It is synthesized and released from endothelial cells and acts upon two receptor subtypes designated as ETA and ETB. In this study, a series of potent dipeptide sulfonamide dual-
Looking for online definition of ETA-R in the Medical Dictionary? ETA-R explanation free. What is ETA-R? Meaning of ETA-R medical term. What does ETA-R mean?
Lethal white syndrome (LWS), also called overo lethal white syndrome (OLWS), lethal white overo (LWO), and overo lethal white foal syndrome (OLWFS), is an autosomal genetic disorder most prevalent in the American Paint Horse. Affected foals are born after the full 11-month gestation and externally appear normal, though they have all-white or nearly all-white coats and blue eyes. However, internally, these foals have a nonfunctioning colon. Within a few hours, signs of colic appear; affected foals die within a few days. Because the death is often painful, such foals often are humanely euthanized once identified. The disease is particularly devastating because foals are born seemingly healthy after being carried to full term. The disease has a similar cause to Hirschsprungs disease in humans. A mutation in the middle of the endothelin receptor type B (EDNRB) gene causes lethal white syndrome when homozygous. Carriers, which are heterozygous-that is, have one copy of the mutated allele, but ...
Although acetylcholine has conventionally been used to estimate endothelial function, it is unlikely that it is a major regulator of basal vascular tone and NO release in vivo. In contrast, ET-1 has been shown to be a potent stimulator of eNOS even at picomolar doses.12 We have reported that ETBR stimulation by BQ-3020, particularly at lower doses, more precisely reflects endothelial function than does ET-1, which also stimulates ETAR on VSMCs.12 However, we further examined the effects of ET-1 in rats with hypercholesterolemia and their controls. ET-1 exerted a vasodilatory effect at lower doses but a vasoconstrictive effect at higher doses and a dose-dependent NO release in the kidneys of control rats but only vasoconstrictive effects in the kidneys of hypercholesterolemic rats. In the previous study, we demonstrated that ET-1 had similar effects in the kidneys of DOCA-salt hypertensive rats. We therefore speculate that the effects of BQ-3020 on vascular tone and NO release, especially at ...
We have developed a tissue-engineering approach for the production of a completely biological blood vessel from cultured human cells. In the present study, we took advantage of this tissue-engineering method to demonstrate that it can be used to reproduce the subtle differences in the expression of receptors present on the media of native human blood vessels. Indeed, a small percentage (3 of 18) of native human umbilical cord veins (HUCVs) responded to endothelin, the most powerful vasopressor agent known to date, via both endothelin A (ETA) and endothelin B (ETB) receptor activation. In contrast, most HUCVs tested responded toETviaETA receptor activation only. Tissue-engineered vascular media (TEVM) were next reconstructed by using vascular smooth muscle cells (VSMCs) isolated and cultured from HUCVs expressing both ETA and ETB receptors to determine the functional integrity of our TEVM model. The reconstructed TEVM presents an endothelin response similar to that of respective HUCVs from which ...
Arterial injury models for coronary artery disease have demonstrated an enhanced expression and function of either the endothelinAor endothelinB (ETA or ETB) receptor subtype. We hypothesized that organ culture would enhance the physiological function of ET receptors in the porcine right coronary artery. Arteries were either cold stored (4°C) or organ cultured (37°C) for 4 days. After 4 days, the artery was either 1) sectioned into rings to measure the ET-1-induced isometric tension response (3 × 10−10-3 × 10−7 M), or 2) enzymatically dispersed and the isolated smooth muscle cells imaged using fura-2 to measure the myoplasmic calcium (Cam) response to 3 × 10−8 M ET-1 (∼EC50). Isometric tension and Cam to ET-1 were measured in the absence and presence of bosentan (nonselective ETA or ETB receptor antagonist), BQ788 (ETB-selective antagonist), and BQ123 (ETA-selective antagonist). Compared with cold storage, organ culture induced a 2-fold increase in tension development (3 × 10−7 M ...
Biological Description: Macitentan(ACT064992) is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).IC50 value: Target: ETA/ETB ...
AequoScreen® Double Transfected Cell Lines: Endothelin, ETB subtype. Human Recombinant, in CHO-K1 host cell. Two vials of cryopreserved cells are shipped per order. A detailed technical dossier includes sequence, culture conditions and pharmacological properties of the recombinant receptor. All cell lines are tested for the absence of mycoplasma. Terms and conditions apply. Some products are not available in some countries. Please inquire at your local sales office for more information.. Features:. ...
Piebald, which is not known to exist in cornsnakes yet, prematurely kills off or deactivates migrating cells. This is responsible for the areas where no color or pattern develop. Several different species are known to have piebald mutants at a locus that corresponds to the same locus in the other species. (The locus is known as the endothelin-B receptor.) As a result, it is very likely that a piebald mutant will appear in cornsnakes someday and create that same phenotype. However, many of the mutants that cause piebaldism also cause severe or lethal effects on homozygotes. As a result, bad piebaldism might be discovered several times in a species before a good version is found ...
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GPR37 antibody (G protein-coupled receptor 37 (endothelin receptor type B-like)) for IHC-P. Anti-GPR37 pAb (GTX85872) is tested in Human samples. 100% Ab-Assurance.
Aspartate mutation distinguishes ETA but not ETB receptor subtype-selective ligand binding while abolishing phospholipase C activation in both receptors.: The e
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Verheij JB, Kunze J, Osinga J, van Essen AJ, Hofstra RM (2002). „ABCD syndrome is caused by a homozygous mutation in the EDNRB gene. Am. J. Med. Genet. 108 (3): 223-5. PMID 11891690. doi:10.1002/ajmg.10172 ...
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You may have seen people mix BCAAs with their pre-workout and wondered, why? Turns out, stacking BCAAs in this way can help improve strength and endurance.