The Full Wiki

More info on Vasopressin receptor antagonist

Vasopressin receptor antagonist: Wikis


Note: Many of our articles have direct quotes from sources you can cite, within the Wikipedia article! This article doesn't yet, but we're working on it! See more info or our list of citable articles.


From Wikipedia, the free encyclopedia

A vasopressin receptor antagonist is an agent which interferes with action at the vasopressin receptors. They can be used in the treatment of hyponatremia, especially in patients with congestive heart failure or liver cirrhosis.[1]




Demeclocycline, a tetracycline antibiotic, is sometimes used to block the action of vasopressin in the kidney in hyponatremia due to inappropriately high secretion of vasopressin (SIADH), when fluid restriction has failed.[2]



A new class of medication, the "vaptan" drugs, act by inhibiting the action of vasopressin on its receptors (V1A, V1B and V2). These receptors have a variety of functions, with the V1A and V2 receptors mainly expressed peripherally and involved in the modulation of blood pressure and kidney function respectively, while the V1B receptor is expressed in the brain and pituitary gland and may be a target for psychiatric drugs.

The vaptan class of drugs contains a number of compounds with varying selectivity, several of which are either already in clinical use or in clinical trials as of 2009.[3][4][5]

Unselective (mixed V1A/V2)
V1A selective
V1B selective
V2 selective


  1. ^ Palm C, Pistrosch F, Herbrig K, Gross P (July 2006). "Vasopressin antagonists as aquaretic agents for the treatment of hyponatremia". Am. J. Med. 119 (7 Suppl 1): S87–92. doi:10.1016/j.amjmed.2006.05.014. PMID 16843091.  
  2. ^ Padfield PL, Hodsman GP, Morton JJ (September 1978). "Demeclocycline in the treatment of the syndrome of inappropriate antidiuretic hormone release: with measurement of plasma ADH". Postgrad Med J 54 (635): 623–7. PMID 103083.  
  3. ^ Serradeil-Le Gal C, Wagnon J, Valette G, Garcia G, Pascal M, Maffrand JP, Le Fur G. Nonpeptide vasopressin receptor antagonists: development of selective and orally active V1a, V2 and V1b receptor ligands. Progress in Brain Research. 2002;139:197-210. PMID 12436936
  4. ^ Lemmens-Gruber R, Kamyar M. Vasopressin antagonists. Cellular and Molecular Life Sciences. 2006 Aug;63(15):1766-79. PMID 16794787
  5. ^ Decaux G, Soupart A, Vassart G. Non-peptide arginine-vasopressin antagonists: the vaptans. Lancet. 2008 May 10;371(9624):1624-32. PMID 18468546


Got something to say? Make a comment.
Your name
Your email address