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The **arginine vasopressin type 2 receptor** (AVPR2, also called vasopressin receptor 2 or V2 receptor) is a G protein-coupled receptor predominantly expressed in the renal collecting duct, where it responds to the neurohypophyseal hormone arginine vasopressin (antidiuretic hormone). Upon stimulation, AVPR2 activates G~s~ proteins, increasing intracellular cAMP, and leads to the insertion of aquaporin-2 water channels into the apical membrane—concentrating urine and maintaining water homeostasis. Additionally, AVPR2 is expressed in other tissues such as endothelial cells, mediating the release of von Willebrand factor and factor VIII. Mutations in AVPR2 underlie X-linked nephrogenic diabetes insipidus, and its inappropriate activation is involved in SIADH and can contribute pathologically to certain cancers (notably clear cell renal carcinoma). Pharmaceuticals targeting AVPR2 include both agonists (for conditions like von Willebrand disease) and antagonists (for hyponatremia and polycystic kidney disease)[1][2][3][4][5][7][8].
Antagonists (e.g., Tolvaptan) block V2R to promote aquaresis (water excretion) and reduce tumor growth/angiogenesis Agonists (e.g., Desmopressin) activate V2R to stimulate water reabsorption and increase levels of coagulation factors (e.g., von Willebrand factor, factor VIII) Modulation of cAMP signaling by activation/inhibition of G~s~-coupled receptor pathways
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