Tolvaptan is a non-peptide aquaretic agent that functions as a selective, competitive vasopressin receptor 2 (v2) antagonist. Aquaretic agents are being studied for water-retaining disorders like congestive heart failure and live cirrhosis.
Tolvaptan has been shown to inhibit the development of polycystic kidney disease in several animal models.
|Application||Tolvaptan has been used as a V2-selective antagonist in mouse models of hypertension.|
|Mechanism of Action||Tolvaptan is a selective, competitive vasopressin receptor 2 (v2) antagonist, 29 times for selective than the vasopressin receptor V1a. It is a derivative of OPC-31260.|
|Eukaryotic Cell Culture Applications||Autosomal dominant polyscystic kidney disease (ADPKD) is the most common inherited renal disorder. Aberrant epithelial cell proliferation is responsible for growth of cysts, which leads to nephron loss, enlarged kidneys, and decline in kidney function. Tolvaptan inhibits renal effects of arginine vasopressin (AVP) and slows cyst growth in animal models. When studying the effect of Tolvaptan using human epithelial cells from an cyst cultured in a 3D matirx, Tolvaptan was found to inhibit AVP-induced Cl− secretion and decreased in vitro cyst growth. (Reif et al, 2011).|
|Solubility||Soluble in methanol and DMSO. Practically insoluble in water.|
|References||Jalal GK, Hamad B, Yasothan U and Kirkpatrick P (2009) Tolvaptan. Nat. Rev. Drug Disc. 8:611-612 Reif GA et al (2011) Tolvaptan inhibits ERK-dependent cell proliferation, Cl- secretion, and in vitro cyst growth of human ADPKD cells stimulated by vasopressin. Am J Physiol Renal Physiol. 301(5):F1005-13 Schrier RW et al (2006) Tolvaptan, a selective oral vasopressin V2 receptor antagonist, for hyponatremia. N. Eng. J. Med. 355:2099-2112|