Quantitative autoradiography was used to characterize angiotensin AT1 and AT2 receptors, in the rat aorta at three developmental ages; embryonic day 18 (E18), and postnatal weeks 2 and 8. The expression of angiotensin receptors was higher in the aorta of E18 and 2-week-old rat. A major proportion of the angiotensin receptors expressed in the aorta at these two ages was AT2 (84 and 81% respectively). Conversely, in the aorta of 8-week-old rats, AT1 was the predominant angiotensin receptor subtype (71%). In 8-week-old rats, the AT2 subtype was also present (28%). In pre- and postnatal rats, [125I]Sar1-angiotensin II binding to AT1 receptors was sensitive to GTP gamma S whereas binding to AT2 receptors was not. AT2 receptors may serve an important role during stages of rapid growth of the aorta, and also have a significant function in the adult vasculature ...
BACKGROUND: Sodium-induced hypertensive cardiac hypertrophy is related to pressure and volume overload. METHODS: Wistar rats were exposed to low and high sodium diet for 8 weeks. Angiotensin II receptor mRNA, abundance of p38 mitogen-activated protei
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The most significant finding of our study is that it establishes, for the first time to our knowledge, that RNAi technology can be used to silence the AT1aR subtype. This provides us with a powerful tool for elucidating the respective roles of AT1aR and AT1bR subtypes in the diverse and profound physiological effects of Ang II in the cardiovascular system in normal animals. The observed reduction in [125I]-Sar1-Ile8 Ang II binding, AT1aR mRNA levels, and Ang II-stimulated [45Ca2+] uptake demonstrates that at least 1 of the 3 dsRNA targeted for the AT1aR subtype is selective and efficient in silencing the AT1aR subtype gene. The dsRNA AT1 47 is more efficient in reducing AT1aR numbers compared with its sister subtype, the AT1bR, despite the fact that these subtypes share 96% similarity. The dsRNA AT1 47 is highly efficient and produces AT1aR silencing that lasts for ≈3 days. Until now, the popular technology to reduce angiotensin receptors has been the use of antisense oligonucleotides.13-18 ...
Section 1 of this thesis contains an introduction to method development in organic synthesis, multicomponent reactions, sulfonyl azides, tracer development in 11C chemistry and the biological target.. Section 2 describes the use of sulfonyl azides in carbonylative chemistry. Paper I covers development of a diazotransfer protocol. In total, 30 arylsulfonyl azides were synthesised from primary sulfonamides (20-90% yield). 15N mechanistic studies were carried out and in Paper II, the products were converted into sulfonamides, sulfonylureas and sulfonyl carbamates (19-90% yield). For ureas and carbamates, a two-chamber protocol was employed to release CO from Mo(CO)6. 15N mechanistic studies showed that the sulfonamides were formed by direct displacement of azide.. Section 3 covers imaging and biological studies of the angiotensin II receptor subtype 2 (AT2R). In Paper III, 12 11C-sulfonyl carbamates were prepared in isolated radiochemical yields of 3-51% via Rh(I)-mediated carbonylation. The first ...
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The angiotensin II receptors, (AGTR1) and (AGTR2), are a class of G protein-coupled receptors with angiotensin II as their ligands. They are important in the renin-angiotensin system: they are responsible for the signal transduction of the vasoconstricting stimulus of the main effector hormone, angiotensin II. The AT1 and AT2 receptors share a sequence identity of ~30%, but have a similar affinity for angiotensin II, which is their main ligand. The AT1 receptor is the best elucidated angiotensin receptor. The AT1 subtype is found in the heart, blood vessels, kidney, adrenal cortex, lung and brain and mediates the vasoconstrictor effects. The angiotensin receptor is activated by the vasoconstricting peptide angiotensin II. The activated receptor in turn couples to Gq/11 and Gi/o and thus activates phospholipase C and increases the cytosolic Ca2+ concentrations, which in turn triggers cellular responses such as stimulation of protein kinase C. Activated receptor also inhibits adenylate cyclase and ...
AVALIDE® (irbesartan-hydrochlorothiazide) is an oral antihypertensive authorities that joins irbesartan, a non-peptide foe of angiotensin II receptor subtype (AT1) with a thiazide diuretic, hydrochlorothiazide. Mexico pharmacy drugs
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Angiotensin II acts through two separate receptors namely AT1 and AT2. Two AT1 receptor subtypes (AT1A and AT1B) have been described. FEBS Lett. 1992 Feb 24;298(2-3):257-60. AT1 receptors are distributed widely in tissues including the adipose tissue as well as vasculature, heart, kidney, brain, liver, adrenal gland and lung. Am J Hypertens. 2000 Jan;13(1 Pt 2):31S-38S. The classic effects of Angiotensin II namely vasoconstriction, as well as aldosterone stimulation from the adrenal gland with sodium and water reabsorption in the kidneys are mediated through the AT1 receptors. Pharmacol Rev. 1993 Jun;45(2):205-51. AT2 receptor expression which is initially widespread in the foetus, decreases post-natally and remains expressed in the adipose tissue as well as the vasculature, heart, adrenal gland, pancreas and female reproductive organs. Am J Hypertens. 2000 Jan;13(1 Pt 2):31S-38S. Angiotensin seems to act on AT2 receptors to produce effects totally opposed to those mediated by the AT1 receptor ...
PubMed journal article: Effect of angiotensin-converting enzyme two-week inhibition on renal angiotensin II receptors and renal vascular reactivity in SHR. Download Prime PubMed App to iPhone, iPad, or Android
Shop Type-1B angiotensin II receptor ELISA Kit, Recombinant Protein and Type-1B angiotensin II receptor Antibody at MyBioSource. Custom ELISA Kit, Recombinant Protein and Antibody are available.
The present study demonstrates that (1) ET-1 and Ang II receptors are present and functional with a cell-specific distribution in adult rat cardiomyocytes and fibroblasts; (2) ET-1 receptor densities and ET-1-induced [Ca2+]i are not altered in adult cardiomyocytes and fibroblasts from hypertrophied hearts; (3) cardiac hypertrophy induces a significant downregulation of Ang II receptors (which are exclusively of the AT1 subtype) on adult fibroblasts, with no alteration in [Ca2+]i sensitivity to Ang II, but reduces efficacy of the [Ca2+]i response; and (4) [Ca2+]i sensitivity to Ang II and Ang II total binding are significantly higher in hypertrophied cardiomyocytes, suggesting upregulation of Ang II receptors. Cultured adult rat cardiomyocytes41 and cardiac fibroblasts27 are good cell models for studying molecular and cellular changes in control and experimental conditions, such as cardiac hypertrophy. As we reported here, on the basis of morphological and biochemical characteristics, the cell ...
https://doi.org/10.18632/oncotarget.24492 Yusuke Ito, Aya Naiki-Ito, Hiroyuki Kato, Shugo Suzuki, Toshiya Kuno, Yukari Ishiguro, Satoru Takahashi, Hiroji Uemura
Previous studies of the physiological functions of Ang IV in the brain have required the direct injection of this peptide in the brain ventricles.12,14,31 In addition to being invasive, this strategy precludes the evaluation of long-term effects of this peptide. To explore the role of chronic elevations of Ang IV in brain, we used a fusion protein capable of targeting the direct release of an Ang IV peptide in the brain. The major finding of the present study is that moderate overproduction of Ang IV peptide in the brain of transgenic mice induced hypertension that could be reversed by an AT1 receptor antagonist. We have ruled out several of the more trivial explanations for this finding: First, the m-Ang IV peptides could display an increased affinity for the AT1 receptor or be produced in such large quantities that they are able to bind and activate the AT1 receptor. This is clearly not the case, however, because the m-Ang IV peptides show no capacity to displace Ang II from the AT1B receptor ...
BioAssay record AID 39364 submitted by ChEMBL: Compound was evaluated for 50% inhibitory concentration against angiotensin II receptor.
The deregulation of the cholinergic system has been implicated in the development of cognitive symptoms associated with mental illnesses, such as Alzheimers disease and schizophrenia (Rainer and Mucke, 1998; Raedler et al., 2007; Langmead et al., 2008). The cholinergic M1AChR receptor subtype is widely expressed in the cortical and limbic brain regions, and extensive evidence indicates a mediating role in cognitive processes (Buckley et al., 1988; Anagnostaras et al., 2003; Conn et al., 2009b). Thus, the M1AChR receptor has emerged as a potential pharmacological target for diseases characterized by cognitive impairment. Unfortunately, the high degree of conservation between muscarinic receptor subtypes at their orthosteric ligand binding sites has hindered the development of M1AChR-selective drugs. The M1/M2/M4AChR-preferring muscarinic agonist xanomeline showed symptom reduction efficacy in patients with both Alzheimers disease and schizophrenia; however, parasympathetic side effects, ...
The angiotensin receptors are seven-membrane G-protein-coupled receptors. They mediate the cardiovascular and other effects of angiotensin II which is a bioactive peptide of the renin-angiotensin system.. ...
Novartis (Basel, Switzerland) new heart failure drug, Entresto, has created a lot of buzz due to its strong efficacy and clinical demand. This first-in-class small molecule drug was fast-tracked due to impressive clinical trial results. Entresto is a combination drug: Valsartan and Sacubitril. They work together to lower blood pressure, which lowers the strain on the heart and lessens the accumulation of fluid in tissues such as the lungs-a key symptom of heart failure. Valsartan is an angiotensin II receptor inhibitor; it stops angiotensin II. Why is stopping angiotensin II important?. Angiotensin II is a small hormone. When it attaches to the angiotensin receptor, it causes a cascade of reactions to occur. That cascade ultimately causes blood vessels to constrict, which causes blood pressure to increase. Think about it like this-it takes more pressure to move a fluid through a narrow tube than through a wide one. Angiotensin II also promotes the release of a second hormone, aldosterone, which ...
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Lactation in the rat is characterized by dramatic changes in the HP axis, as well as a more than doubling in food and water intake, compared with nonlactating rats (30). All of these physiological changes are necessary for the successful rearing of the pups. The RAS is a well-characterized regulator of several HP axis systems, as well as fluid and electrolyte balance. Therefore, changes in ANG II receptor expression in the hypothalamus during lactation could potentially explain some of the physiological changes that occur in this reproductive state.. Prl secretion is critical for milk production. In view of the demonstrated ability of brain ANG II to inhibit Prl secretion via stimulation of DA neuronal activity and release (20, 29) from the ARH and ME, respectively, successful milk production during lactation may entail a reduction in ANG II-mediated DA release from these regions. Therefore, the significant decrease in ANG II binding in ARH of the lactating rat (Table 1; Fig. 1, G andH) is ...
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
Finally, we review future possible drug discovery in terms of Ang II receptor regulation, focusing on "activation of physiological function". Activation of the AT2 receptor is expected to have various beneficial effects on not only the cardiovascular system but also other organ disorders; however, there is no appropriate AT2 receptor-agonist available. CGP42112A, which has been used as an AT2 receptor agonist thus far, also has antagonistic effects at higher concentrations. Therefore, a highly agonistic drug for AT2 receptor activation that is widely available is awaited for elucidation of the roles of the AT2 receptor in the pathogenesis of cardiovascular disease. The results of overexpression studies of the AT2 receptor could be quite different from the physiological function of the receptor, because expression of the AT2 receptor is generally lower in adult normal tissues and the AT2 receptor would be transactivated in response to some stimuli such vascular injury. Moreover, the exact ...
November 6, 2018, admin Angiotensin Receptors, Many viral proteins undergo proteolytic processing events that are necessary for virus infection and virion assembly. WNV NS3 was suggested to process mainly NS2ANS2BNS3NS4A at combined basic proteins occupying the P1 and P2 positions. Certainly, purified NS3 was discovered to cleave the anthrax toxinprotective antigen PA83 [3], whereas the furin/PC-like pentapeptide fluorogenic substrate Pyr-RTKR-MCA [PyroGlu-Arg-Thr-Lys-Arg-(4-methylcoumarin-7-amide)] […]. 13463-28-0 IC50, Rabbit Polyclonal to JAB1. ...
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Angiotensin receptor 1 (AT1 receptor) is a member of angiotensin receptors which are responsible for the signal transduction of the main effecter hormone.
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A receptor antagonist is a chemical that binds to a receptor of a cell, but does not trigger a response by that cell. Antagonists have affinity towards binding to the receptors they target, but no efficacy to activate the receptor.[1][2] Receptor antagonists have no activity in the absence of a receptor agonist; however, the binding of a receptor antagonist will disrupt the interaction and inhibit the function of an agonist or inverse agonist at receptors.
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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 ...
TY - JOUR. T1 - Downregulation of vascular angiotensin II type 1 receptor by thyroid hormone. AU - Fukuyama, Kae. AU - Ichiki, Toshihiro. AU - Takeda, Kotaro. AU - Tokunou, Tomotake. AU - Iino, Naoko. AU - Masuda, Satoko. AU - Ishibashi, Minako. AU - Egashira, Kensuke. AU - Shimokawa, Hiroaki. AU - Hirano, Katsuya. AU - Kanaide, Hideo. AU - Takeshita, Akira. PY - 2003/3/1. Y1 - 2003/3/1. N2 - Thyroid hormone has a broad effect on cardiovascular system. 3,3′,5-triiodo-L-thyronine (T3), a biologically active form of thyroid hormone, increases cardiac contractility. T3 causes arterial relaxation and reduction of systemic vascular resistance, resulting in an increase in cardiac output. However, the molecular mechanisms of vascular relaxation by T3 are incompletely characterized. We studied the effect of T3 on the angiotensin (Ang) II type 1 receptor (AT1R) expression in vascular smooth muscle cells. T3 dose-dependently decreased expression levels of AT1R mRNA, with a peak at 6 hours of ...
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.