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Vasopressin receptor 2 (V2R), or arginine vasopressin receptor 2 (officially called AVPR2), is a protein that acts as receptor for vasopressin. [5] AVPR2 belongs to the subfamily of G-protein-coupled receptors. Its activity is mediated by the G s type of G proteins, which stimulate adenylate cyclase.
Tolvaptan, sold under the brand name Samsca among others, is an aquaretic drug that functions as a selective, competitive vasopressin receptor 2 (V 2) antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH).
Lixivaptan (VPA-985) is an orally-active, non-peptide, selective vasopressin 2 receptor antagonist being developed as an investigational drug by Palladio Biosciences, Inc. (Palladio), a subsidiary of Centessa Pharmaceuticals plc.
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.
Vasopressin receptor antagonists (VRAs) are drugs that block vasopressin receptors. Most commonly VRAs are used to treat hyponatremia caused by syndrome of inappropriate antidiuretic hormone secretion (SIADH), congestive heart failure (CHF) and cirrhosis. [2] Somatostatin is a competitive inhibitor. [5]
Inhibits vasopressin secretion Water: Inhibits vasopressin secretion Acidifying salts: calcium chloride, ammonium chloride: 1. Arginine vasopressin receptor 2 antagonists: amphotericin B, lithium [13] [14] Inhibits vasopressin's action 5. collecting duct: Selective vasopressin V2 antagonist (sometimes called aquaretics) tolvaptan, [15] conivaptan
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 ...
It also participates in calcium regulation by reabsorbing Ca 2+ in response to parathyroid hormone. [1] PTH effect is mediated through phosphorylation of regulatory proteins and enhancing the synthesis of all transporters within the distal convoluted tubule. Arginine vasopressin receptor 2 is also expressed in the DCT.