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Arginine Vasopressin Receptor 2
Vasopressin receptor 2 (V2R), or arginine vasopressin receptor 2 (officially called AVPR2), is a protein that acts as receptor for vasopressin. AVPR2 belongs to the subfamily of G-protein-coupled receptors. Its activity is mediated by the Gs type of G proteins, which stimulate adenylate cyclase. AVPR2 is expressed in the kidney tubule, predominantly in the membrane of cells of the distal convoluted tubule and collecting ducts, in fetal lung tissue and lung cancer, the last two being associated with alternative splicing. AVPR2 is also expressed outside the kidney in vascular endothelium.Jackson EK (2018). "Drugs Affecting Renal Excretory Function". In: Brunton LL, Hilal-Dandan R, Knollmann BC. eds. ''Goodman & Gilman's: The Pharmacological Basis of Therapeutics'', 13e New York, NY: McGraw-Hill. Stimulation causes the release of von Willebrand factor and factor VIII from the endothelial cells. Because von Willebrand factor helps stabilize circulating levels of factor VIII, the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residue (biochemistry), residues. Proteins perform a vast array of functions within organisms, including Enzyme catalysis, catalysing metabolic reactions, DNA replication, Cell signaling, responding to stimuli, providing Cytoskeleton, structure to cells and Fibrous protein, organisms, and Intracellular transport, transporting molecules from one location to another. Proteins differ from one another primarily in their sequence of amino acids, which is dictated by the Nucleic acid sequence, nucleotide sequence of their genes, and which usually results in protein folding into a specific Protein structure, 3D structure that determines its activity. A linear chain of amino acid residues is called a polypeptide. A protein contains at least one long polypeptide. Short polypeptides, containing less than 20–30 residues, are rarely considered to be proteins and are commonly called pep ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hemophilia A
Haemophilia A (or hemophilia A) is a blood clotting disorder caused by a genetic deficiency in clotting factor VIII, thereby resulting in significant susceptibility to bleeding, both internally and externally. This condition occurs almost exclusively in males born to carrier mothers due to X-linked recessive inheritance. Nevertheless, rare isolated cases do emerge from de novo (spontaneous) mutations. The medical management of individuals with hemophilia A frequently entails the administration of factor VIII medication through slow intravenous injection. This intervention aims to address and preempt additional bleeding episodes in affected individuals. Signs and symptoms Haemophilia A's phenotype has a quite wide range of symptoms encompassing both internal and external bleeding episodes. Individuals with more severe haemophilia tend to experience more intense and frequent bleeding, whereas those with mild haemophilia typically exhibit milder symptoms unless subjected to sur ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Syndrome Of Inappropriate Antidiuretic Hormone
Syndrome of inappropriate antidiuretic hormone secretion (SIADH), also known as the syndrome of inappropriate antidiuresis (SIAD), is characterized by a physiologically inappropriate release of antidiuretic hormone (ADH) either from the posterior pituitary gland, or an ectopic non-pituitary source, such as an ADH-secreting tumor in the lung. Unsuppressed ADH causes a physiologically inappropriate increase in solute-free water being reabsorbed by the tubules of the kidney to the venous circulation leading to hypotonic hyponatremia (a low plasma osmolality and low sodium levels). The causes of SIADH are commonly grouped into categories including: central nervous system diseases that directly stimulate the hypothalamus to release ADH, various cancers that synthesize and secrete ectopic ADH, various lung diseases, numerous drugs (carbamazepine, cyclophosphamide, SSRIs) that may stimulate the release of ADH, vasopressin release, desmopressin release, oxytocin, or stimulation of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hyponatremia
Hyponatremia or hyponatraemia is a low concentration of sodium in the Serum (blood), blood. It is generally defined as a sodium concentration of less than 135 mmol/L (135 mEq/L), with severe hyponatremia being below 120 mEq/L. Symptoms can be absent, mild or severe. Mild symptoms include a Altered level of consciousness, decreased ability to think, headaches, nausea, and Balance disorder, poor balance. Severe symptoms include confusion, seizures, and coma; death can ensue. The causes of hyponatremia are typically classified by a person's body fluid status into hypovolemic, low volume, normal volume, or hypervolemic, high volume. Low volume hyponatremia can occur from diarrhea, vomiting, diuretics, and sweating. Normal volume hyponatremia is divided into cases with concentration, dilute urine and concentration, concentrated urine. Cases in which the urine is dilute include adrenal insufficiency, hypothyroidism, and polydipsia, drinking too much water or potomania, t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Satavaptan
Satavaptan (INN; developmental code name SR121463, former tentative brand name Aquilda) is a vasopressin V2 receptor antagonist which was investigation by Sanofi-Aventis and was under development for the treatment of hyponatremia. It was also being studied for the treatment of ascites Ascites (; , meaning "bag" or "sac") is the abnormal build-up of fluid in the abdomen. Technically, it is more than 25 ml of fluid in the peritoneal cavity, although volumes greater than one liter may occur. Symptoms may include increased abdo .... Development was discontinued in 2009. References Diuretics Tert-butyl compounds Vasopressin receptor antagonists Benzamides 4-Morpholinyl compounds Ethanolamines Cyclohexanols Spiro compounds Sulfonamides Ethoxy compounds Lactams Methoxy compounds {{cardiovascular-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mozavaptan
Mozavaptan (INN) is a vasopressin receptor antagonist marketed by Otsuka. In Japan, it was approved in October 2006 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone Syndrome of inappropriate antidiuretic hormone secretion (SIADH), also known as the syndrome of inappropriate antidiuresis (SIAD), is characterized by a physiologically inappropriate release of antidiuretic hormone (ADH) either from the posterio ... (SIADH) due to ADH producing tumors. References * * Diuretics Benzanilides Benzazepines Vasopressin receptor antagonists 2-Tolyl compounds {{antihypertensive-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lixivaptan
Lixivaptan (VPA-985) is an orally-active, non-peptide, selective vasopressin V2 receptor antagonist being developed as an investigational drug by Palladio Biosciences, Inc. (Palladio), a subsidiary of Centessa Pharmaceuticals plc. , lixivaptan is in phase III clinical development for the treatment of autosomal dominant polycystic kidney disease (ADPKD), the most common form of polycystic kidney disease. The U.S. Food and Drug Administration (FDA) has granted orphan drug designation to lixivaptan for the treatment of ADPKD. Mechanism of action Lixivaptan is a potent, non-peptide, selective vasopressin receptor antagonist. It is a member of the vaptan class of drugs. Hyponatremia V2 receptor antagonists inhibit the binding of arginine vasopressin to vasopressin receptor 2 (V2R) in kidney tubular epithelial cells, thereby having a net effect of aquaresis, or electrolyte free water excretion. This property of vaptans explains their use as therapies to treat euvolemic and hyper ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Food And Drug Administration (United States)
The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food safety, tobacco products, caffeine products, dietary supplements, prescription and over-the-counter pharmaceutical drugs (medications), vaccines, biopharmaceuticals, blood transfusions, medical devices, electromagnetic radiation emitting devices (ERED), cosmetics, animal foods & feed and veterinary products. The FDA's primary focus is enforcement of the Federal Food, Drug, and Cosmetic Act (FD&C). However, the agency also enforces other laws, notably Section 361 of the Public Health Service Act as well as associated regulations. Much of this regulatory-enforcement work is not directly related to food or drugs but involves other factors like regulating lasers, cellular phones, and condoms. In addition, the FDA takes control of disea ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tolvaptan
Tolvaptan, sold under the brand name Samsca among others, is an aquaretic drug that functions as a selective, competitive antagonist, competitive vasopressin receptor antagonist, vasopressin receptor 2 (V2) antagonist used to treat hyponatremia (low blood sodium levels) associated with heart failure, congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Tolvaptan was approved by the U.S. Food and Drug Administration (FDA) on May 19, 2009, and is sold by Otsuka Pharmaceutical Co. under the trade name Samsca. Tolvaptan, as Jynarque, was granted approval for medical use in the United States in April 2018. The U.S. Food and Drug Administration (FDA) granted tolvaptan a Fast track (FDA), fast track designation for clinical trials investigating its use for the treatment of polycystic kidney disease. The FDA granted Jynarque an orphan drug designation in April 2012, for the treatment of autosomal dominant polycystic kidney disease. Tolvapta ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vasopressin Receptor Antagonist
A vasopressin receptor antagonist (VRA) is an agent that interferes with action at the vasopressin receptors. Most commonly VRAs are used in the treatment of hyponatremia, especially in patients with congestive heart failure, liver cirrhosis or SIADH. Types Vaptans The "vaptan" drugs act by directly blocking the action of vasopressin at its receptors ( V1A, V1B and V2). These receptors have a variety of functions, with the V1A and V2 receptors are expressed peripherally and involved in the modulation of blood pressure and kidney function respectively, while the V1A and V1B receptors are expressed in the central nervous system. V1A is expressed in many regions of the brain, and has been linked to a variety of social behaviors in humans and animals. The vaptan class of drugs contains a number of compounds with varying selectivity, several of which are either already in clinical use or in clinical trials as of 2009. ;Unselective (mixed V1A/V2) * Conivaptan ;V1A selective ( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Homeostasis
In biology, homeostasis (British English, British also homoeostasis; ) is the state of steady internal physics, physical and chemistry, chemical conditions maintained by organism, living systems. This is the condition of optimal functioning for the organism and includes many variables, such as body temperature and fluid balance, being kept within certain pre-set limits (homeostatic range). Other variables include the pH of extracellular fluid, the concentrations of sodium, potassium, and calcium ions, as well as the blood sugar level, and these need to be regulated despite changes in the environment, diet, or level of activity. Each of these variables is controlled by one or more regulators or homeostatic mechanisms, which together maintain life. Homeostasis is brought about by a natural resistance to change when already in optimal conditions, and equilibrium is maintained by many regulatory mechanisms; it is thought to be the central motivation for all organic action. All home ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
