Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.
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Here we present a protocol to image cells expressing green fluorescent protein-tagged angiotensin type 1a receptors during endocytosis...
https://doi.org/10.18632/oncotarget.24492 Yusuke Ito, Aya Naiki-Ito, Hiroyuki Kato, Shugo Suzuki, Toshiya Kuno, Yukari Ishiguro, Satoru Takahashi, Hiroji Uemura
Complete information for AGTR1 gene (Protein Coding), Angiotensin II Receptor Type 1, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
Complete information for AGTR2 gene (Protein Coding), Angiotensin II Receptor Type 2, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
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Angiotensin II receptor type 1 or AT1 receptor is the best characterized angiotensin receptor. It has vasopressor effects and regulates aldosterone secretion. It is an important effector controlling blood pressure and volume in the cardiovascular system. Angiotensin II receptor antagonists are drugs indicated for hypertension, diabetic nephropathy and congestive heart failure. The AT1 receptor mediates the major cardiovascular effects of angiotensin II. Effects include vasoconstriction, aldosterone synthesis and secretion, increased vasopressin secretion, cardiac hypertrophy, augmentation of peripheral noradrenergic activity, vascular smooth muscle cells proliferation, decreased renal blood flow, renal renin inhibition, renal tubular sodium reuptake, modulation of central sympathetic nervous system activity, cardiac contractility, central osmocontrol and extracellular matrix formation. The angiotensin receptor is activated by the vasoconstricting peptide angiotensin II. The activated receptor in ...
Angiotensin II receptor type 2, also known as the AT2 receptor is a protein that in humans is encoded by the AGTR2 gene. Angiotensin II is a potent pressor hormone and a primary regulator of aldosterone secretion. It is an important effector controlling blood pressure and volume in the cardiovascular system. It acts through at least two types of receptors termed AT1 and AT2. AGTR2 belongs to a family 1 of G protein-coupled receptors. It is an integral membrane protein. It plays a role in the central nervous system and cardiovascular functions that are mediated by the renin-angiotensin system. This receptor mediates programmed cell death (apoptosis). In adults, it is highly expressed in myometrium with lower levels in adrenal gland and fallopian tube. It is highly expressed in fetal kidney and intestine. The human AGTR2 gene is composed of three exons and spans at least 5 kb. Exons 1 and 2 encode for 5 untranslated mRNA sequence and exon 3 harbors the entire uninterrupted open reading frame. ...
TY - JOUR. T1 - Reactive oxygen species and cyclooxygenase 2-derived thromboxane A2 reduce angiotensin II type 2 receptor vasorelaxation in diabetic rat resistance arteries. AU - Retailleau, Kevin. AU - Belin De Chantemèle, Eric J.. AU - Chanoine, Sébastien. AU - Guihot, Anne Laure. AU - Vessières, Emilie. AU - Toutain, Bertrand. AU - Faure, Sébastien. AU - Bagi, Zsolt. AU - Loufrani, Laurent. AU - Henrion, Daniel. PY - 2010/2. Y1 - 2010/2. N2 - Angiotensin II has a key role in the control of resistance artery tone and local blood flow. Angiotensin II possesses 2 main receptors. Although angiotensin II type 1 receptor is well known and is involved in the vasoconstrictor and growth properties of angiotensin II, the role of the angiotensin II type 2 receptor (AT2R) remains much less understood. Although AT2R stimulation induces vasodilatation in normotensive rats, it induces vasoconstriction in pathological conditions involving oxidative stress and cyclooxygenase 2 expression. Thus, we studied ...
Over the last 2 decades, it has become clear that angiotensin can be generated not only in the systemic circulation but also in multiple tissue sites, where its production can be regulated by local factors. Given the ability of angiotensin II to influence target cell proliferation, hypertrophy, and apoptosis, tissue angiotensin systems potentially play an important role in a wide variety of physiological processes. In this issue of Hypertension, De Mello and Danser1 review the evidence for the synthesis of angiotensin II in the heart and discuss its possible role in health and disease. Their review complements other recent reviews of this subject, such as that by Dostal and Baker.2 Uniquely, however, the present review discusses the potential role of intracellular angiotensin II, called intracrine angiotensin II, in intercellular signaling and calcium flux in the heart. These findings are based on De Mellos studies1 of renin, angiotensin I, and angiotensin II dialyzed into rat cardiac cells. ...
293445024 - EP 1091966 B1 2002-11-06 - N-TERMINAL SITE SELECTIVE INHIBITORS OF HUMAN ANGIOTENSIN CONVERSION ENZYME (ACE) - [origin: WO0001706A1] The invention concerns peptide derivatives useful as N-terminal site selective inhibitor of the human angiotensin conversion enzyme. Said derivatives comprise the amino acid sequence of the following formula: -Asp-Phe- psi (PO2CH2)-Ala-Xaa - wherein: psi (PO2CH2) indicates that the peptide bond (CONH) between Phe and Ala has been replaced by the phosphonic bond PO2CH2; and Xaa represents an amino acid residue. Said derivatives can be used in pharmaceutical compositions, in particular for protecting hematopoietic strain cells of patients subjected to aggressive chemotherapeutic or radiotherapy treatment.[origin: WO0001706A1] The invention concerns peptide derivatives useful as N-terminal site selective inhibitor of the human angiotensin conversion enzyme. Said derivatives comprise the amino acid sequence of the following formula: -Asp-Phe- psi (PO2CH2)-Ala-Xaa
Angiotensin II is a potent pressor hormone and a primary regulator of aldosterone secretion. It is an important effector controlling blood pressure and volume in the cardiovascular system. It acts through at least two types of receptors termed AT1 and AT2. AGTR2 belongs to a family 1 of G protein-coupled receptors. It is an integral membrane protein. It plays a role in the central nervous system and cardiovascular functions that are mediated by the renin-angiotensin system. This receptor mediates programmed cell death (apoptosis). In adults, it is highly expressed in myometrium with lower levels in adrenal gland and fallopian tube. It is highly expressed in fetal kidney and intestine. The human AGTR2 gene is composed of three exons and spans at least 5 kb. Exons 1 and 2 encode for 5 untranslated mRNA sequence and exon 3 harbors the entire uninterrupted open reading frame.[1] Stimulation of AT2 by the selective agonist CGP 42112A increases mucosal nitric oxide production.[2] ...
The angiotensin II type I receptor (AGTR1) has a strong influence on tumor growth, angiogenesis, inflammation and immunity. However, the role of AGTR1 on lymph node metastasis (LNM) in breast cancer, which correlates with tumor progression and patient survival, has not been examined. AGTR1 was highly expressed in lymph node-positive tumor tissues, which was confirmed by the Oncomine database. Next, inhibition of AGTR1 reduced tumor growth and LNM in orthotopic xenografts by bioluminescence imaging (BLI). Losartan, an AGTR1-specific inhibitor, decreased the chemokine pair CXCR4/SDF-1α levels in vivo and inhibited AGTR1-induced cell migration and invasion in vitro. Finally, the molecular mechanism of AGTR1-induced cell migration and LNM was assessed by knocking down AGTR1 in normal cells or CXCR4 in AGTR1high cells. AGTR1-silenced cells treated with losartan showed lower CXCR4 expression. AGTR1 overexpression caused the upregulation of FAK/RhoA signaling
This gene encodes a transmembrane protein localized to the plasma membrane and perinuclear vesicular structures. The gene product interacts with the angiotensin II type I receptor and negatively regulates angiotensin II signaling. Alternative splicing of this gene generates multiple transcript variants encoding different isoforms. [provided by RefSeq, Jul 2008 ...
We studied the effects of intravenous infusion of angiotensin II on the circulation of the fetus in lambs in utero through chronically maintained intravascular catheters. Angiotensin II infused in doses of 29-280 ng/min per kg fetal weight resulted in an increase in plasma angiotensin II from a control value of 87 +/- 17 to 341 +/- 129 (mean +/- SE) pg/ml; these levels are similar to those observed following hemorrhage in fetal lambs. Fetal mean arterial blood pressure increased from 46 +/- 2.0 to 56 +/- 2.7 torr and fetal heart rate increased from 172 +/- 6 to 189 +/- 6 beats/min, an effect which was not altered by beta-adrenergic or cholinergic blockade. Fetal cardiac output and its distribution were measured before and during infusion of angiotensin II by the radionuclide-labeled microsphere technique. Combined ventricular output increased significantly from 526 +/- 32 to 616 +/- 24 ml/min per kg fetal body weight. Angiotensin constricted the umbilical-placental circulation as well as the ...
Studies on the effects of angiotensin AT1-receptor antagonists and angiotensin AT2-receptor agonists and the combination thereof on vascular tone in mouse mesenteric ...
The 1166 A/C polymorphism of the angiotensin II type 1 receptor gene does not correlate with the blood pressure response to angiotensin II in patients with CHF Academic Article ...
The rennin-angiotensin II system (RAS) and the insulin-PI3kinase signalling pathways cross-interact with important physiological and pathophysiological consequences for cells and the whole organism. Here, the effect of 24 h pre-incubation of EA.hy926 with two different concentrations of angiotensin II, on insulin-mediated activation of the PI3kinase-AKT-eNOS signalling was investigated. Quiescent EA.hy926 cells were treated with insulin (100 nM, 30 min) following 24 h pre-treatment with or without either 0.1 or 1 µM of angiotensin II. Cell lysates were immunoblotted for phospho AKT Ser-473, phospho eNOS Ser-1177 and normalized with β-actin. Homogenates of EA.hy926 treated with insulin in the presence or absence of 1 µM angiotensin II, were also subjected to nitric oxide synthase (NOS) activity assay using titrated arginine as substrate. To exclude cytotoxicity of the 1 µM angiotensin II concentration, Trypan blue cell viability assay as well as the microscopic examination of
Radcliffe Cardiology article authored by Tonje A Aksnes covering topics - Angiotensin-converting enzyme inhibitors, angiotensin II type I receptor blockers, atrial fibrillation & on other cardiology field
Top performende anti-Schwein Angiotensin II Type 2 Receptor Antikörper für Immunohistochemistry (Paraffin-embedded Sections) (IHC (p)) vergleichen & kaufen.
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TY - JOUR. T1 - Angiotensin II relaxes microvessels via the AT 2 receptor and Ca 2+ -activated K + (BK Ca ) channels AU - Dimitropoulou, Christiana. AU - White, Richard E.. AU - Fuchs, Leslie. AU - Zhang, Hanfang. AU - Catravas, John D.. AU - Carrier, Gerald O.. PY - 2001/1/1. Y1 - 2001/1/1. N2 - Angiotensin II (Ang II) is one of the most potent vasoconstrictor substances, yet paradoxically. Ang II may dilate certain vascular beds via an undefined mechanism. Ang II-induced vasoconstriction is mediated by the AT 1 receptor, whereas the relative expression and functional importance of the AT 2 receptor in regulating vascular resistance and blood pressure are unknown. We now report that Ang II induces relaxation of mesenteric microvessels and that this vasodilatory response was unaffected by losartan, an AT 1 receptor antagonist, but was inhibited by PD123.319. a selective antagonist of AT 2 receptors. In addition, reverse transcriptase-polymerase chain reaction studies revealed high amounts of AT ...
Hypercholesterolemia and an activated renin-angiotensin-aldosterone system are well-established independent cardiovascular risk factors. Several lines of evidence support an important role of modified LDLs and angiotensin II in the development and progression of atherosclerosis. Angiotensin II is not only a potent vasoconstrictor, but it also promotes proinflammatory and prothrombotic properties of vascular cells. A growing body of in vitro studies shows the induction of cellular adhesion molecules and cytokines by angiotensin II in endothelial cells.1 In vivo, angiotensin II promotes leukocyte-endothelial cell interaction in the microcirculation. This proinflammatory mechanism involves the redox-sensitive mobilization of adhesion molecules such as P-selectin.2,3 These and several additional findings in cell systems and large vessels support a crucial role of the angiotensin II type-1 (AT1) receptor-mediated formation of reactive oxygen species (ROS) in the pathogenesis of atherosclerosis.4,5 ...
Angiotensin convertaza, cunoscuta si sub numele de kinaza II sau peptidil-dipeptidaza A, este o enzima din clasa hidrolazelor implicate in hidroliza legaturilor peptidice la nivelul C-terminal. Are localizare transmembranara si este alcatuita dintr-un singur lant polipeptidic cu doua situsuri catalitice ce contin zinc. Clivajul proteolitic elibereaza din membrana celulara in spatiul extracelular enzima functionala, circulanta6.. Majoritatea angiotensin convertazei (~90%) se gaseste legata in tesuturi si doar o mica parte circula libera in plasma. Sursa principala a enzimei este endoteliul pulmonar.. Enzima participa in cascada sistemului renina-angiotensina-aldosteron ca raspuns la hipovolemie, fiind responsabila de conversia angiotensinei I in angiotensina II, vasoconstrictor puternic care creste tensiunea arteriala. De asemenea angiotensin convertaza este responsabila si de inactivarea bradikininei (in sistemul kalikreina-kinina)3;6.. Activitatea angiotensin convertazei este crescuta in ...
CM has been studied extensively over the past two decades.5,8,11,15-19 Its induction is attenuated by AT1 receptor blockers, ACE inhibitors,9,20 and ICa,L blockade.10 Although little is known about the signaling pathways involved, downstream changes in ion channels that regulate cardiac electrical activity have been described. As one example, induction of CM by ventricular pacing is associated with reduction of the phase 1 action potential notch, Ito, and mRNA for Kv4.3.8,13 Moreover, Ito-blocking drugs suppress CM induction.6 Interestingly, in independent experiments, angiotensin II has been implicated in the modulation of Ito.20. Assuming there is linkage between angiotensin II, calcium, and CM, what we have lacked is an understanding of pathways connecting the upstream factors (eg, AT1 receptors, ICa,L) and the downstream changes in ion channels. In this study, we focused on a portion of a possible signaling pathway, by testing the hypothesis that an important transcription factor in neuronal ...
It is well established that renal hypoxia is associated with the development of renal injury. The purpose of this study is measure the alterations in renal blood oxygenation after angiotensin II converting enzyme inhibition. The understanding of kidney adaptive mechanisms to renin angiotensin system effects in healthy subjects will be useful for the early detection of renal disease and for the development of new therapies to decrease the progression of the disease and its consequences ...
The goal of our study was to determine whether H3Rs afford cardioprotection in I/R by counteracting the AT1R-mediated stimulation of NHE. We found that activation of neuronal H3R opposes the deleterious effects of locally formed ANG II, not only by inhibiting NHE, but also by reducing the expression of AT1R. This novel phenomenon broadens the known cardioprotective effects of H3R activation (Levi and Smith, 2000; Mackins and Levi, 2000).. We had reported previously that H3Rs are activated in I/R and limit the release of pathological amounts of NE and associated reperfusion arrhythmias by decreasing NHE activation, thus counteracting a pivotal mechanism of nonvesicular, carrier-mediated NE release (Levi and Smith, 2000). Because ANG II is formed locally in the heart during I/R (Mackins et al., 2006) and ANG II is a major NHE activator (Reid et al., 2004), we assumed that in I/R the activation of H3R could counterbalance the NHE-stimulating effect of ANG II. Indeed, we found that pharmacological ...
an antihypertensive drug that blocks the formation of angiotensin II in the kidney, leading to relaxation of the arteries; promotes the excretion of salt and water by inhibiting the activity of the angiotensin converting enzyme; also used to treat congestive heart failure. ...
Alamandine | [Ala1]-Angiotensin (1-7), Angiotensin A (1-7) (Human, Rat, Mouse)4475-v 0.5 mg | 25.00 EURAla-Arg-Val-Tyr-Ile-His-Pro (M.W.
Side Effects for GIAPREZA (angiotensin ii injection) are also known as adverse reactions. Below is a summary of known side effects for Giapreza.
In the present study, we showed that ANG II markedly reduced ACE2 in cultured rat VSMCs through a regulatory process mediated by the angiotensin type 1 (AT1) receptor. Treatment of VSMCs with ANG-(1-7), the product of ACE2 hydrolysis of ANG II, did not affect ACE2 mRNA; however, ANG-(1-7) prevented the ANG II-mediated reduction in ACE2 mRNA. Addition of [d-Ala7]-ANG-(1-7), a selective AT(1-7) receptor antagonist, blocked the inhibitory actions of ANG-(1-7). These data are the first to demonstrate opposing transcriptional regulation of ACE2 by ANG II and ANG-(1-7) in VSMCs and suggest a complex interplay between these two peptides that is mediated by distinct receptor pathways. ANG-(1-7) prevented the ANG II-mediated reduction in VSMC ACE2 mRNA, and the inhibitory action of the heptapeptide was blocked by the addition of [d-Ala7]-ANG-(1-7). Since ACE2 preferentially converts ANG II to ANG-(1-7), downregulation of the enzyme by ANG II constitutes a positive feedback system that may favor ANG ...
The purpose of this study is to define the dose for a Phase II study and to investigate safety and tolerability of intravenous administration of recombi
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Mengidentifikasi Peptida Bioaktif Angiotensin Converting Enzyme-inhibitor (ACEi) dari Kasein β Susu Kambing dengan Polimorfismenya Melalui Teknik In Silico
Angiotensin converting enzyme, or ACE, inhibitors slow an enzyme in the body from producing angiotensin II, states Mayo Clinic. Angiotensin II narrows blood vessels and releases hormones that can...
Identifikasi Polimorfisme Insersi/Delesi Gen Angiotensin Converting Enzym Intron 16 Pada Pasien Preeklampsia di RS. Dr. Muhammad Hoesin Palembang
The table below shows the top 100 pain related interactions that have been reported for angiotensin type II receptor activity. They are ordered first by their pain relevance and then by number of times they were reported for angiotensin type II receptor activity. Please click on the INT link to display more detailed information on each interaction. ...
We have been giving importance to the health, security of our employees and management of environment by working in conformity with the codes and the necessities of wavin Group and adobting the understanding of human at first. We give importance to the health, security of our employees and management of environment by working in conformity with the codes and the necessities of wavin Group and adobting the understanding of human at first. We believe that the long term success of our compnay will realize the management of our own work peroformance as well by suitably managing the social and environmental relations.. ...
Protein extracts (50 mg) ended up subjected to immunoblot evaluation with antibodies against Pak1 (Mobile signal, one:one thousand, Mobile Signalling
Mice, Patients, Human, Gene, Cells, Liver, Mouse, Treatment, Cell, Heart, Administration, Angiotensin Ii, Brain, Genes, Angiotensin, Insulin, mRNA, Hypertrophy, Glucose, Metabolism
New Report on Angiotensin II Receptor Type 1 (AT1 Receptor) Inhibitors-Pipeline Insights, 2017 added to fshlxkc.cn store which has 60 pages and available for purchase at US $ 1250.
1. When the renin-angiotensin system of rats had been suppressed by a high salt diet or by bilateral nephrectomy, large doses of angiotensin II antiserum were required to block the pressor action of exogenous angiotensin II. Infusion of renin profoundly lowered the blocking requirement of such animals.. 2. It is postulated that renin bound to blood vessels generates angiotensin locally which is taken up by vascular receptors. Where such receptors are left unoccupied and free to bind exogenous angiotensin, high doses of blocking antisera are required.. 3. Animals with hypertension produced by renal artery constriction with contralateral nephrectomy were shown to be in positive sodium balance. Nevertheless their blocking requirement was low.. 4. It is suggested that the local generation of angiotensin may play a role in the production of renal hypertension and that this accounts for the development of hypertension even in animals immunized against angiotensin. ...
Angiotensin I is converted to angiotensin II (AII) through removal of two C-terminal residues by the enzyme angiotensin-converting enzyme (ACE), primarily through ACE within the lung (but also present in endothelial cells, kidney epithelial cells, and the brain). Angiotensin II acts on the CNS to increase ADH production, and also acts on venous and arterial vessels smooth muscle to cause vasoconstriction. Angiotensin II also increases Aldosterone secretion, therefore, it acts as an endocrine, autocrine/paracrine, and intracrine hormone.. ACE is a target of ACE inhibitor drugs, which decrease the rate of Angiotensin II production. Angiotensin II increases blood pressure by stimulating the Gq protein in vascular smooth muscle cells (which in turn activates an IP3-dependent mechanism leading to a rise in intracellular calcium levels and ultimately causing contraction). In addition, angiotensin II acts at the Na/H+ exchanger in the proximal tubules of the kidney to stimulate Na reabsorption and H+ ...
We identified an angiotensin-generating system in pancreatic islets and found that exogenously administered angiotensin II, after binding to its receptors (angiotensin II type 1 receptor [AT1R]), inhibits insulin release in a manner associated with decreased islet blood flow and (pro)insulin biosynthesis. The present study tested the hypothesis that there is a change in AT1R expression in the pancreatic islets of the obesity-induced type 2 diabetes model, the db/db mouse, which enables endogenous levels of angiotensin II to impair islet function. Islets from 10-week-old db/db and control mice were isolated and investigated. In addition, the AT1R antagonist losartan was administered orally to 4-week-old db/db mice for an 8-week period. We found that AT1R mRNA was upregulated markedly in db/db islets and double immunolabeling confirmed that the AT1R was localized to beta-cells. Losartan selectively improved glucose-induced insulin release and (pro)insulin biosynthesis in db/db islets. Oral ...
1. Competitive or non-competitive inhibition of the myotropic and pressor response of angiotensin II is dependent on the nature of the substituent in position 8 of the antagonist peptide analogue. Substituents in other positions of the molecule, particularly position 1, contribute greatly to the potency of these antagonists.. 2. As is evidenced after adrenalectomy or after blockade with phentolamine and phenoxybenzamine, the initial pressor activity observed with all the antagonistic peptides is partially due to the release of catecholamines and partially to a direct myotropic effect.. 3. [Sar1, Thr8]angiotensin II has been found to possess the lowest agonist to antagonist ratio of all antagonists tested.. 4. [Des-Asp1, Ile8]angiotensin II selectively and specifically inhibits the release of aldosterone from adrenal cortex. Thus, unlike angiotensin II, this heptapeptide has pronounced organ specificity, suggesting that the heptapeptide (angiotensin III) is the aldosterone-releasing ...
Agents that antagonize ANGIOTENSIN II TYPE 1 RECEPTOR. Included are ANGIOTENSIN II analogs such as SARALASIN and biphenylimidazoles such as LOSARTAN. Some are used as ANTIHYPERTENSIVE AGENTS ...
The latest market report published by Credence Research, Inc. "Global Angiotensin Converting Enzyme (ACE) Inhibitors Market - Growth, Share, Opportunities, Competitive Analysis, and Forecast, 2016 - 2022," the angiotensin converting enzyme (ACE) inhibitors market was valued at USD 11,477.1 Mn in 2015, and is expected to reach USD 11,094.6 Mn by 2023, expanding at a CAGR of (0.5%) from 2016 to 2023.. Browse the full report Angiotensin Converting Enzyme (ACE) Inhibitors Market - Growth, Share, Opportunities, Competitive Analysis, and Forecast, 2016 - 2023 report at http://www.credenceresearch.com/report/angiotensin-converting-enzyme-ace-inhibitors-market. Market Insights. ACE inhibitors are class of drugs (angiotensin-converting enzyme inhibitors) that block the conversion of angiotensin I to angiotensin II, used in the treatment of hypertension and congestive heart failure and in the prevention of microvascular complications of diabetes mellitus. According to World Health Organization (WHO), ...
Compare & find the top performing anti-Mouse (Murine) Angiotensin II Type-1 Receptor antibody for Immunohistochemistry (Paraffin-embedded Sections) (IHC (p)).
... definition, any of three oligopeptides occurring in plasma, an inactive form (angiotensin I) and two varieties (angiotensin II and angiotensin III) that elevate blood pressure and stimulate the adrenal cortex to secrete aldosterone. See more.