The Sound of Evolution
Tolvaptan
Mechanism of action:
Tolvaptan is a selective vasopressin V2 receptor antagonist. Tolvaptan selectively antagonizes V2 receptors, which are Gs protein-coupled receptors, on principal cells of the renal collecting ducts. This prevents arginine vasopressin from binding to the receptor and inhibits the translocation of aquaporin-2 to the luminal membrane of the collecting duct, leading to a marked reduction in water reabsorption.
Reference(s):
1. Gheorghiade M et al. (2005). Pharmacology of new agents for acute heart failure syndromes. Am J Cardiol.
2. Ambrosy A et al. (2011). Tolvaptan for the treatment of heart failure: a review of the literature. Expert Opin Pharmacother.
3. Yi S et al. (2012). Pharmacokinetics and pharmacodynamics of oral tolvaptan administered in 15- to 60-mg single doses to healthy Korean men. J Cardiovasc Pharmacol.