V2 receptor antagonism with tolvaptan in heart failure

Lisa C. Costello-Boerrigter, Guido Boerrigter, John C. Burnett

Research output: Contribution to journalReview articlepeer-review

1 Scopus citations


The prevalence and incidence of congestive heart failure continues to increase. The two hallmarks of this syndrome, sodium and water retention, are frequently a therapeutic challenge. Most conventional diuretics act primarily as saluretics by inhibiting renal tubular electrolyte reabsorption, which, due to osmotic pressure, promotes excretion of isotonic fluid. The peptide hormone arginine vasopressin vasoconstricts at the V1A receptor and promotes water reabsorption via the V2 receptor in the renal collecting duct by inserting aquaporin-2 water channels into the luminal membrane. Tolvaptan, the first orally available non-pepticle V2 receptor antagonist, acts as a potent aquaretic. In this paper, the authors review the pharmacology of tolvaptan and discuss the results of the initial clinical trials with this potent new drug.

Original languageEnglish (US)
Pages (from-to)1639-1647
Number of pages9
JournalExpert Opinion on Investigational Drugs
Issue number10
StatePublished - Oct 2007


  • Aquaretic
  • Arginine vasopressin
  • Heart failure
  • Pharmacology
  • Tolvaptan
  • Vasopressin-2 receptor antagonist

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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