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Conivaptan, sold under the brand name Vaprisol, is a non-peptide inhibitor of the receptor for anti-diuretic hormone, also called vasopressin. It was approved in 2004 for hyponatremia (low blood sodium levels). The compound was discovered by Astellas and marked in 2006. The drug is now marketed by Cumberland Pharmaceuticals, Inc.
Vasopressin agonists are used therapeutically in various conditions, and its long-acting synthetic analogue desmopressin is used in conditions featuring low vasopressin secretion, as well as for control of bleeding (in some forms of von Willebrand disease and in mild haemophilia A) and in extreme cases of bedwetting by children.
The actions of vasopressin are mediated by stimulation of tissue-specific G protein-coupled receptors (GPCRs) called vasopressin receptors that are classified into the V 1 (V 1A), V 2, and V 3 (V 1B) receptor subtypes. [1] These three subtypes differ in localization, function and signal transduction mechanisms. [2]
551 11998 Ensembl ENSG00000101200 ENSMUSG00000037727 UniProt P01185 P35455 RefSeq (mRNA) NM_000490 NM_009732 RefSeq (protein) NP_000481 NP_033862 Location (UCSC) Chr 20: 3.08 – 3.08 Mb Chr 2: 130.42 – 130.42 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Human vasopressin, also called antidiuretic hormone (ADH), arginine vasopressin (AVP) or argipressin, is a hormone synthesized ...
Classification of common diuretics and their mechanisms of action. Class Examples Mechanism Location (numbered in distance along nephron) Ethanol: drinking alcohol: Inhibits vasopressin secretion Water: Inhibits vasopressin secretion Acidifying salts: calcium chloride, ammonium chloride: 1. Arginine vasopressin receptor 2 antagonists ...
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The "vaptan" drugs act by directly blocking the action of vasopressin at its receptors (V 1A, V 1B and V 2).These receptors have a variety of functions, with the V 1A and V 2 receptors are expressed peripherally and involved in the modulation of blood pressure and kidney function respectively, while the V 1A and V 1B receptors are expressed in the central nervous system.
Central diabetes insipidus, recently renamed arginine vasopressin deficiency (AVP-D), [1] is a form of diabetes insipidus that is due to a lack of vasopressin (ADH) production in the brain. Vasopressin acts to increase the volume of blood (intravascularly), and decrease the volume of urine produced.