A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.
An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.
Angiotensin-Converting Enzyme Inhibitors
A class of drugs whose main indications are the treatment of hypertension and heart failure. They exert their hemodynamic effect mainly by inhibiting the renin-angiotensin system. They also modulate sympathetic nervous system activity and increase prostaglandin synthesis. They cause mainly vasodilation and mild natriuresis without affecting heart rate and contractility.
Receptor, Angiotensin, Type 1
Receptor, Angiotensin, Type 2
Angiotensin Receptor Antagonists
Angiotensin II Type 1 Receptor Blockers
A BLOOD PRESSURE regulating system of interacting components that include RENIN; ANGIOTENSINOGEN; ANGIOTENSIN CONVERTING ENZYME; ANGIOTENSIN I; ANGIOTENSIN II; and angiotensinase. Renin, an enzyme produced in the kidney, acts on angiotensinogen, an alpha-2 globulin produced by the liver, forming ANGIOTENSIN I. Angiotensin-converting enzyme, contained in the lung, acts on angiotensin I in the plasma converting it to ANGIOTENSIN II, an extremely powerful vasoconstrictor. Angiotensin II causes contraction of the arteriolar and renal VASCULAR SMOOTH MUSCLE, leading to retention of salt and water in the KIDNEY and increased arterial blood pressure. In addition, angiotensin II stimulates the release of ALDOSTERONE from the ADRENAL CORTEX, which in turn also increases salt and water retention in the kidney. Angiotensin-converting enzyme also breaks down BRADYKININ, a powerful vasodilator and component of the KALLIKREIN-KININ SYSTEM.
A peptidyl-dipeptidase that catalyzes the release of a C-terminal dipeptide, -Xaa-*-Xbb-Xcc, when neither Xaa nor Xbb is Pro. It is a Cl(-)-dependent, zinc glycoprotein that is generally membrane-bound and active at neutral pH. It may also have endopeptidase activity on some substrates. (From Enzyme Nomenclature, 1992) EC 220.127.116.11.
Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.
The active metabolite of ENALAPRIL and a potent intravenously administered angiotensin-converting enzyme inhibitor. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.
1-Sarcosine-8-Isoleucine Angiotensin II
A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.
Rats, Inbred SHR
An alpha-globulin of about 453 amino acids, depending on the species. It is produced by the liver and secreted into blood circulation. Angiotensinogen is the inactive precursor of natural angiotensins. Upon successive enzyme cleavages, angiotensinogen yields angiotensin I, II, and III with amino acids numbered at 10, 8, and 7, respectively.
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.
Rats, Inbred WKY
A generic term used to describe a group of polypeptides with related chemical structures and pharmacological properties that are widely distributed in nature. These peptides are AUTACOIDS that act locally to produce pain, vasodilatation, increased vascular permeability, and the synthesis of prostaglandins. Thus, they comprise a subset of the large number of mediators that contribute to the inflammatory response. (From Goodman and Gilman's The Pharmacologic Basis of Therapeutics, 8th ed, p588)
Dose-Response Relationship, Drug
Drug Therapy, Combination
Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.
Calcium Channel Blockers
Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.
Mineralocorticoid Receptor Antagonists
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.
Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.
A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827)
KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE.
Abnormally high potassium concentration in the blood, most often due to defective renal excretion. It is characterized clinically by electrocardiographic abnormalities (elevated T waves and depressed P waves, and eventually by atrial asystole). In severe cases, weakness and flaccid paralysis may occur. (Dorland, 27th ed)
Receptor, Bradykinin B2
A constitutively expressed subtype of bradykinin receptor that may play a role in the acute phase of the inflammatory and pain response. It has high specificity for intact forms of BRADYKININ and KALLIDIN. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.
Glomerular Filtration Rate
Rats, Inbred Strains
Disease Models, Animal
Sodium Chloride Symporter Inhibitors
Sympathetic Nervous System
The thoracolumbar division of the autonomic nervous system. Sympathetic preganglionic fibers originate in neurons of the intermediolateral column of the spinal cord and project to the paravertebral and prevertebral ganglia, which in turn project to target organs. The sympathetic nervous system mediates the body's response to stressful situations, i.e., the fight or flight reactions. It often acts reciprocally to the parasympathetic system.
A free radical gas produced endogenously by a variety of mammalian cells, synthesized from ARGININE by NITRIC OXIDE SYNTHASE. Nitric oxide is one of the ENDOTHELIUM-DEPENDENT RELAXING FACTORS released by the vascular endothelium and mediates VASODILATION. It also inhibits platelet aggregation, induces disaggregation of aggregated platelets, and inhibits platelet adhesion to the vascular endothelium. Nitric oxide activates cytosolic GUANYLATE CYCLASE and thus elevates intracellular levels of CYCLIC GMP.
Hypertrophy, Left Ventricular
A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)
Kidney Failure, Chronic
The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.
21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.
Enzyme that is a major constituent of kidney brush-border membranes and is also present to a lesser degree in the brain and other tissues. It preferentially catalyzes cleavage at the amino group of hydrophobic residues of the B-chain of insulin as well as opioid peptides and other biologically active peptides. The enzyme is inhibited primarily by EDTA, phosphoramidon, and thiorphan and is reactivated by zinc. Neprilysin is identical to common acute lymphoblastic leukemia antigen (CALLA Antigen), an important marker in the diagnosis of human acute lymphocytic leukemia. There is no relationship with CALLA PLANT.
Atrial Natriuretic Factor
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Hydroxymethylglutaryl-CoA Reductase Inhibitors
NG-Nitroarginine Methyl Ester
Cardiac Output, Low
A state of subnormal or depressed cardiac output at rest or during stress. It is a characteristic of CARDIOVASCULAR DISEASES, including congenital, valvular, rheumatic, hypertensive, coronary, and cardiomyopathic. The serious form of low cardiac output is characterized by marked reduction in STROKE VOLUME, and systemic vasoconstriction resulting in cold, pale, and sometimes cyanotic extremities.
Analysis of Variance
A flavoprotein enzyme that catalyzes the univalent reduction of OXYGEN using NADPH as an electron donor to create SUPEROXIDE ANION. The enzyme is dependent on a variety of CYTOCHROMES. Defects in the production of superoxide ions by enzymes such as NADPH oxidase result in GRANULOMATOUS DISEASE, CHRONIC.
Antidiuretic hormones released by the NEUROHYPOPHYSIS of all vertebrates (structure varies with species) to regulate water balance and OSMOLARITY. In general, vasopressin is a nonapeptide consisting of a six-amino-acid ring with a cysteine 1 to cysteine 6 disulfide bridge or an octapeptide containing a CYSTINE. All mammals have arginine vasopressin except the pig with a lysine at position 8. Vasopressin, a vasoconstrictor, acts on the KIDNEY COLLECTING DUCTS to increase water reabsorption, increase blood volume and blood pressure.
Kidney Tubules, Proximal
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care. (Dictionary of Health Services Management, 2d ed)
A complex of cells consisting of juxtaglomerular cells, extraglomerular mesangium lacis cells, the macula densa of the distal convoluted tubule, and granular epithelial peripolar cells. Juxtaglomerular cells are modified SMOOTH MUSCLE CELLS found in the walls of afferent glomerular arterioles and sometimes the efferent arterioles. Extraglomerular mesangium lacis cells are located in the angle between the afferent and efferent glomerular arterioles. Granular epithelial peripolar cells are located at the angle of reflection of the parietal to visceral angle of the renal corpuscle.
Receptor, Bradykinin B1
A subtype of BRADYKININ RECEPTOR that is induced in response to INFLAMMATION. It may play a role in chronic inflammation and has a high specificity for KININS lacking the C-terminal ARGININE such as des-Arg(10)-kallidin and des-Arg(9)-bradykinin. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.
Ventricular Dysfunction, Left
A condition in which the LEFT VENTRICLE of the heart was functionally impaired. This condition usually leads to HEART FAILURE; MYOCARDIAL INFARCTION; and other cardiovascular complications. Diagnosis is made by measuring the diminished ejection fraction and a depressed level of motility of the left ventricular wall.
Nitric Oxide Synthase
Studies comparing two or more treatments or interventions in which the subjects or patients, upon completion of the course of one treatment, are switched to another. In the case of two treatments, A and B, half the subjects are randomly allocated to receive these in the order A, B and half to receive them in the order B, A. A criticism of this design is that effects of the first treatment may carry over into the period when the second is given. (Last, A Dictionary of Epidemiology, 2d ed)
Ventricular Function, Left
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
Studies used to test etiologic hypotheses in which inferences about an exposure to putative causal factors are derived from data relating to characteristics of persons under study or to events or experiences in their past. The essential feature is that some of the persons under study have the disease or outcome of interest and their characteristics are compared with those of unaffected persons.
Highly reactive compounds produced when oxygen is reduced by a single electron. In biological systems, they may be generated during the normal catalytic function of a number of enzymes and during the oxidation of hemoglobin to METHEMOGLOBIN. In living organisms, SUPEROXIDE DISMUTASE protects the cell from the deleterious effects of superoxides.
Randomized Controlled Trials as Topic
Reactive Oxygen Species
Molecules or ions formed by the incomplete one-electron reduction of oxygen. These reactive oxygen intermediates include SINGLET OXYGEN; SUPEROXIDES; PEROXIDES; HYDROXYL RADICAL; and HYPOCHLOROUS ACID. They contribute to the microbicidal activity of PHAGOCYTES, regulation of signal transduction and gene expression, and the oxidative damage to NUCLEIC ACIDS; PROTEINS; and LIPIDS.
Kidney Function Tests
Renal Artery Obstruction
Proteolytic enzymes from the serine endopeptidase family found in normal blood and urine. Specifically, Kallikreins are potent vasodilators and hypotensives and increase vascular permeability and affect smooth muscle. They act as infertility agents in men. Three forms are recognized, PLASMA KALLIKREIN (EC 18.104.22.168), TISSUE KALLIKREIN (EC 22.214.171.124), and PROSTATE-SPECIFIC ANTIGEN (EC 126.96.36.199).
Type 2 diabetes
"Effect of angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers on all-cause mortality, cardiovascular ... "Relation of active, passive, and quitting smoking with incident type 2 diabetes: a systematic review and meta-analysis". The ... There is some evidence that angiotensin converting enzyme inhibitors (ACEIs) are superior to other inhibitors of the renin- ... angiotensin system such as angiotensin receptor blockers (ARBs), or aliskiren in preventing cardiovascular disease. ...
... is also thought to be the cause of the dry cough in some patients on widely prescribed angiotensin-converting enzyme ... Icatibant is one such inhibitor. Additional bradykinin inhibitors exist. It has long been known in animal studies that ... Bradykinin is a physiologically and pharmacologically active peptide of the kinin group of proteins, consisting of nine amino ... In humans, bradykinin is broken down by three kininases: angiotensin-converting enzyme (ACE), aminopeptidase P (APP), and ...
"Design of specific inhibitors of angiotensin-converting enzyme: new class of orally active antihypertensive agents". Science. ... Captopril, sold under the brand name Capoten among others, is an angiotensin-converting enzyme (ACE) inhibitor used for the ... "Angiotensin-converting enzyme inhibitors". Circulation. 97 (14): 1411-20. doi:10.1161/01.cir.97.14.1411. PMID 9577953.. ... "High-resolution crystal structures of Drosophila melanogaster angiotensin-converting enzyme in complex with novel inhibitors ...
... an enzyme that normally inactivates circulating cortisol to the less-active metabolite cortisone. At high concentrations ... Instead, extremely high levels of the precursor hormone corticosterone are produced, some of which is converted to 11- ... Experiments show that treatment with Spironolactone (an inhibitor of the aldosterone receptor), does not prevent hypertension ... that decreased perfusion of renal tissue due to stenosis of a main or branch renal artery activates the renin-angiotensin ...
Angiotensin-converting enzyme. 3.4.16. *Serine type carboxypeptidases: Cathepsin A. *DD-transpeptidase ... In general, they have two highly conserved aspartates in the active site and are optimally active at acidic pH. Nearly all ... Pepstatin is an inhibitor of aspartate proteases. Classification. Five superfamilies (clans) of aspartic proteases are ... Aspartic proteases are a catalytic type of protease enzymes that use an activated water molecule bound to one or more aspartate ...
Diabetes mellitus type 2
"Effect of angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers on all-cause mortality, cardiovascular ... "Relation of active, passive, and quitting smoking with incident type 2 diabetes: a systematic review and meta-analysis". The ... Angiotensin-converting enzyme inhibitors (ACEIs) prevent kidney disease and improve outcomes in those with diabetes. ... dipeptidyl peptidase-4 inhibitors, SGLT2 inhibitors, and glucagon-like peptide-1 analogs. There is no significant ...
Renin converts angiotensinogen (inactive form) to angiotensin I (active form).. *Angiotensin I flows in the bloodstream until ... it reaches the capillaries of the lungs where angiotensin converting enzyme (ACE) acts on it to convert it into angiotensin II. ... the RAS is targeted pharmacologically by ACE inhibitors and angiotensin II receptor antagonists, also known as angiotensin ... Renin-angiotensin system (RAS): This system is generally known for its long-term adjustment of arterial pressure. This system ...
... via a series of enzymes. The last hydrolysis that releases the active oxytocin nonapeptide is catalyzed by peptidylglycine ... Mizutani S, Yokosawa H, Tomoda Y (July 1992). "Degradation of oxytocin by the human placenta: effect of selective inhibitors". ... its C-terminus has been converted to a primary amide and a disulfide bridge joins the cysteine moieties. Oxytocin has a ... The biologically active form of oxytocin, commonly measured by RIA and/or HPLC techniques, is also known as the octapeptide " ...
Azole antifungal drugs (except for abafungin) inhibit the enzyme lanosterol 14 α-demethylase; the enzyme necessary to convert ... renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists. *Renin inhibitors. *Antihyperlipidemics * ... Ciclopirox - (ciclopirox olamine) - is a hydroxypyridone antifungal that interferes with active membrane transport, cell ... Orotomide (F901318) - pyrimidine synthesis inhibitor.. *Miltefosine disrupts fungal cell membrane dynamics by ...
Proteasome endopeptidase complex
Angiotensin-converting enzyme. 3.4.16. *Serine type carboxypeptidases: Cathepsin A. *DD-transpeptidase ... is an enzyme. This enzyme catalyses the following chemical reaction ... Active site. *Binding site. *Catalytic triad. *Oxyanion hole. *Enzyme promiscuity. *Catalytically perfect enzyme ...
... (marketed under the brand name Accupril by Pfizer) is an angiotensin-converting enzyme inhibitor (ACE inhibitor) used ... it is converted to its active metabolite, quinaprilat, in the liver. Quinapril inhibits angiotensin converting enzyme, an ... enzyme which catalyses the formation of angiotensin II from its precursor, angiotensin I. Angiotensin II is a powerful ... Due to reduced angiotensin production, plasma concentrations of aldosterone are also reduced, resulting in increased excretion ...
These include the angiotensin-converting enzyme inhibitor captopril. Captopril is based on the peptidic bradykinin potentiating ... Extracts of some natural products led to modern discovery of their active ingredients and eventually to the development of new ... Enzymes in turn are composed of amino acids and often non-peptidic cofactors that are essential for enzyme function. The basic ... In animals, the three carbon precursors lactate or glycerol can be converted into pyruvate which in turn can be converted into ...
آنزیم ۲ مبدل آنژیوتانسین - ویکیپدیا، دانشنامهٔ آزاد
... is a novel mammalian metallocarboxypeptidase and a homologue of angiotensin-converting enzyme insensitive to ACE inhibitors". ... "A novel angiotensin-converting enzyme-related carboxypeptidase (ACE2) converts angiotensin I to angiotensin 1-9". Circulation ... "A novel angiotensin-converting enzyme-related carboxypeptidase (ACE2) converts angiotensin I to angiotensin 1-9". Circulation ... Angiotensin-converting enzyme 2. ». در دانشنامهٔ ویکیپدیای انگلیسی.. برای مطالعهٔ بیشتر[ویرایش]. *. Turner AJ, Hiscox JA, ...
Prostaglandin DP2 receptor
Enzyme. (inhibitors). COX. (PTGS). *Salicylic acids: Aloxiprin. *Aspirin (acetylsalicylic acid). *Benorilate (benorylate) ... Ligands that activate DP2 stimulate the in vitro chemotaxis (i.e. directed migration) of leukocytes active in mediating ... and adenyl cyclase converts AMP into cyclic AMP (cAMP) thereby down-regulating cAMP-responsive proteins involved in cell ... Setipiprant (ACT-129968), a selective, orally active antagonist of the (DP2) receptor, proved to be well-tolerated and ...
Not to be confused with Acetylcholinesterase inhibitor.. An angiotensin-converting-enzyme inhibitor (ACE inhibitor) is a ... ACE inhibitors were used as the active treatment in seven trials (n=76,615) and angiotensin receptor blocker (ARB) in 13 trials ... ACE (Angiotensin converting enzyme) then removes a further two residues, converting angiotensin I into angiotensin II. ACE is ... "Treatment with low-dose angiotensin-converting enzyme inhibitor (ACEI) plus angiotensin II receptor blocker (ARB) in pediatric ...
Angiotensin-converting enzyme. 3.4.16. *Serine type carboxypeptidases: Cathepsin A. *DD-transpeptidase ... A class of oral hypoglycemics called dipeptidyl peptidase-4 inhibitors work by inhibiting the action of this enzyme, thereby ... 2bgn: HIV-1 TAT PROTEIN DERIVED N-TERMINAL NONAPEPTIDE TRP2-TAT (1-9) BOUND TO THE ACTIVE SITE OF DIPEPTIDYL PEPTIDASE IV (CD26 ... The protein encoded by the DPP4 gene is an antigenic enzyme expressed on the surface of most cell types and is associated with ...
renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists. *Renin inhibitors. *Antihyperlipidemics * ... This drug has been reported to reduce the frequency of regulatory T cells (T-Reg) and after converting from a CNI monotherapy ... These drugs may raise the risk of contracting tuberculosis or inducing a latent infection to become active. Infliximab and ... which is a key enzyme in the de novo guanosine nucleotide synthesis. In contrast to other human cell types, lymphocytes B and T ...
... angiotensin converting enzyme inhibitors (ACEIs) improve outcomes in those with DM while the similar medications angiotensin ... Willi C, Bodenmann P, Ghali WA, Faris PD, Cornuz J (December 2007). "Active smoking and the risk of type 2 diabetes: a ... "Effect of angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers on all-cause mortality, cardiovascular ...
Angiotensin-converting enzyme. 3.4.16. *Serine type carboxypeptidases: Cathepsin A. *DD-transpeptidase ... Inhibitors. Main articles: Protease inhibitor (biology) and Protease inhibitor (pharmacology). The activity of proteases ... Some proteases are less active after autolysis (e.g. TEV protease) whilst others are more active (e.g. trypsinogen). ... Enzyme is shown in black, substrate protein in red and water in blue.The top panel shows 1-step hydrolysis where the enzyme ...
The enzyme tyrosine hydroxylase converts tyrosine to L-DOPA in the first step of catecholamine synthesis. L-DOPA is then ... which starts a cascade of reactions that lead to formation of angiotensin II. Angiotensin receptors in cells of the zona ... The HPA axis is an example of a negative feedback system, in which cortisol itself acts as a direct inhibitor of both CRH and ... the biologically active hormone. ... noradrenaline is converted to epinephrine by the enzyme ...
Hormonal breast enhancement
... the epidermal growth factor receptor through specific E-prostanoid receptors and tumor necrosis factor-alpha converting enzyme ... de Pedro M, Baeza S, Escudero MT, Dierssen-Sotos T, Gómez-Acebo I, Pollán M, Llorca J (2015). "Effect of COX-2 inhibitors and ... orally active, growth hormone (GH) secretagogue, MK-677, on 24-hour GH profiles, insulin-like growth factor I, and ... "The Procognitive and Synaptogenic Effects of Angiotensin IV-Derived Peptides Are Dependent on Activation of the Hepatocyte ...
... the enzymes that convert these precursor molecules into insulin and IAPP, respectively, are not able to keep up with the high ... Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: D2 ... After this the transformation from the precursor protein proIAPP to the biologically active IAPP is complete (IAPP sequence: ... Amylin is degraded in part by insulin-degrading enzyme. Receptors. There appear to be at least three distinct ...
... and some may also play a role in blood pressure through inhibition of the angiotensin-converting enzyme (ACE), as well as ... are centrally active in vivo". Peptides. 10 (4): 747-51. doi:10.1016/0196-9781(89)90107-1. PMID 2587417.. ... "Hemorphins derived from hemoglobin have an inhibitory action on angiotensin converting enzyme activity". FEBS Letters. 287 (1-2 ... Enkephalinase inhibitors: Amastatin. *BL-2401. *Candoxatril. *D -Phenylalanine. *Dexecadotril (retorphan). *Ecadotril ( ...
... and angiotensin converting enzyme inhibitors. The severity is divided into mild (5.5-5.9 mmol/L), moderate (6.0-6.4 mmol/L ... There is active excretion of potassium in the distal tubule and the collecting duct; both are controlled by aldosterone. In ... Examples of medications are: ACE inhibitors, angiotensin receptor blockers, and calcineurin inhibitor immunosuppressants ... Desai, A (14 October 2008). "Hyperkalemia associated with inhibitors of the renin-angiotensin-aldosterone system: balancing ...
ACE inhibitors-inhibitors of angiotensin-converting enzyme are often used to reduce the formation of the more potent ... It is believed that angiotensin I may have some minor activity, but angiotensin II is the major bio-active product. Angiotensin ... Angiotensin I is then converted to an octapeptide, angiotensin II by angiotensin-converting enzyme (ACE), which is thought ... Angiotensin I is subsequently converted to angiotensin II by the angiotensin-converting enzyme (ACE) found on the surface of ...
Angiotensin-converting enzyme. 3.4.16. *Serine type carboxypeptidases: Cathepsin A. *DD-transpeptidase ... Cathepsin A is an enzyme that is classified both as a cathepsin and a carboxypeptidase. In humans, it is encoded by the CTSA ... enzyme activator activity. • hydrolase activity. • exo-alpha-sialidase activity. • serine-type carboxypeptidase activity. ... This gene encodes a glycoprotein that associates with lysosomal enzymes beta-galactosidase and neuraminidase to form a complex ...
Nonsteroidal anti-inflammatory drug
For some drugs (typically profens), an isomerase enzyme in vivo converts the inactive enantiomer into the active form, although ... Kidney failure is especially a risk if the patient is also concomitantly taking an ACE inhibitor (which removes angiotensin ... Most NSAIDs act as nonselective inhibitors of the enzyme cyclooxygenase (COX), inhibiting both the cyclooxygenase-1 (COX-1) and ... NSAIDs work by inhibiting the activity of cyclooxygenase enzymes (COX-1 and/or COX-2). In cells, these enzymes are involved in ...
... angiotensin converting enzyme inhibitors or angiotensin receptor blockers along with beta blockers are recommended. For ... First-line therapy for people with heart failure due to reduced systolic function should include angiotensin-converting enzyme ... Active ischemia. *Angina pectoris *Prinzmetal's angina. *Stable angina. *Acute coronary syndrome *Myocardial infarction ... an enzyme which catalyses the production of the potent vasopressor angiotensin. Angiotensin and its metabolites cause further ...
Luteinizing hormone/choriogonadotropin receptor
It specifically acts to up-regulate the enzyme cholesterol side chain cleaving enzyme, which leads to the greater conversion of ... The binding of LH (or CG) to the receptor shifts the equilibrium between active and inactive receptors. LH and LH-agonists ... as the fetal Leydig cells produce androstenedione which is converted to testosterone in fetal Sertoli cells to induce ... Aromatase inhibitors (e.g., anastrozole). *GnRH agonists (e.g., GnRH). Antigonadotropins. *Sex steroid agonists (via negative ...
Enzymes can be targeted with enzyme inhibitors. Receptors are typically categorised based on structure and function. Major ... Metabolism - Is the API converted chemically inside the body, and into which substances. Are these active (as well)? Could they ... Adenosine reuptake inhibitor (AdoRI). *Angiotensin II receptor antagonist. *Endothelin receptor antagonist. *NK1 receptor ... When describing the pharmacokinetic properties of the chemical that is the active ingredient or active pharmaceutical ...