BIOMAT Database Logo BIOMAT Database Logo

Vasopressin V2 receptor antagonists. 2002

J G Verbalis
232 Building D, Division of Endocrinology and Metabolism, Georgetown University School of Medicine, 4000 Reservoir Road NW, Washington DC 20007, USA. verbalis@georgetown.edu

Hyponatremia, whether due to the syndrome of inappropriate antidiuretic hormone secretion (SIADH) or disorders of water retention such as congestive heart failure and cirrhosis, is a very common problem encountered in the care of medical patients. To date, available treatment modalities for disorders of excess arginine vasopressin (AVP) secretion or action have been limited and suboptimal. The recent discovery and development of nonpeptide AVP V(2) receptor antagonists represents a promising new treatment option to directly antagonize the effects of elevated plasma AVP concentrations at the level of the renal collecting ducts. By decreasing the water permeability of renal collecting tubules, excretion of retained water is promoted, thereby normalizing or improving hypo-osmolar hyponatremia. In this review, SIADH and other water retaining disorders are briefly discussed, after which the published preclinical and clinical studies of several nonpeptide AVP V(2) receptor antagonists are summarized. The likely therapeutic indications and potential complications of these compounds are also described.

UI MeSH Term Description Entries
D007177 Inappropriate ADH Syndrome A condition of HYPONATREMIA and renal salt loss attributed to overexpansion of BODY FLUIDS resulting from sustained release of ANTIDIURETIC HORMONES which stimulates renal resorption of water. It is characterized by normal KIDNEY function, high urine OSMOLALITY, low serum osmolality, and neurological dysfunction. Etiologies include ADH-producing neoplasms, injuries or diseases involving the HYPOTHALAMUS, the PITUITARY GLAND, and the LUNG. This syndrome can also be drug-induced. Antidiuretic Hormone, Inappropriate Secretion,Inappropriate Vasopressin Secretion Syndrome,SIADH,Schwartz-Bartter Syndrome,Syndrome of Inappropriate ADH (SIADH) Secretion,ADH Syndrome, Inappropriate,Schwartz Bartter Syndrome,Syndrome, Inappropriate ADH,Syndrome, Schwartz-Bartter
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001127 Arginine Vasopressin The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE. Argipressin,Vasopressin, Arginine,Arg-Vasopressin,Argipressin Tannate,Arg Vasopressin
D017483 Receptors, Vasopressin Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors. Antidiuretic Hormone Receptors,Receptors, V1,Receptors, V2,V1 Receptors,V2 Receptors,Vasopressin Receptors,8-Arg-Vasopressin Receptor,Antidiuretic Hormone Receptor,Antidiuretic Hormone Receptor 1a,Antidiuretic Hormone Receptor 1b,Arginine Vasopressin Receptor,Argipressin Receptor,Argipressin Receptors,Receptor, Arginine(8)-Vasopressin,Renal-Type Arginine Vasopressin Receptor,V1 Receptor,V1a Vasopressin Receptor,V1b Vasopressin Receptor,V2 Receptor,Vascular-Hepatic Type Arginine Vasopressin Receptor,Vasopressin Receptor,Vasopressin Receptor 1,Vasopressin Type 1A Receptor,Vasopressin V1a Receptor,Vasopressin V1b Receptor,Vasopressin V2 Receptor,Vasopressin V3 Receptor,8 Arg Vasopressin Receptor,Hormone Receptor, Antidiuretic,Hormone Receptors, Antidiuretic,Receptor, Antidiuretic Hormone,Receptor, Arginine Vasopressin,Receptor, Argipressin,Receptor, V1,Receptor, V2,Receptor, Vasopressin,Receptor, Vasopressin V1b,Receptor, Vasopressin V3,Receptors, Antidiuretic Hormone,Receptors, Argipressin,Renal Type Arginine Vasopressin Receptor,V1b Receptor, Vasopressin,Vascular Hepatic Type Arginine Vasopressin Receptor,Vasopressin Receptor, V1b
D065092 Antidiuretic Hormone Receptor Antagonists Endogenous compounds and drugs that inhibit or block the activity of ANTIDUIRETIC HORMONE RECEPTORS. Antidiuretic Hormone Antagonist,Antidiuretic Hormone Receptor Antagonist,Vasopressin Antagonist,Vasopressin Receptor Antagonist,Antidiuretic Hormone Antagonists,Vasopressin Antagonists,Vasopressin Receptor Antagonists,Antagonist, Antidiuretic Hormone,Antagonist, Vasopressin,Antagonist, Vasopressin Receptor,Antagonists, Antidiuretic Hormone,Antagonists, Vasopressin,Antagonists, Vasopressin Receptor,Hormone Antagonist, Antidiuretic,Hormone Antagonists, Antidiuretic,Receptor Antagonist, Vasopressin,Receptor Antagonists, Vasopressin

Related Publications

J G Verbalis
Vasopressin V2-receptor antagonists: panaceas for hyponatremia?
September 1997, Current opinion in nephrology and hypertension,
J G Verbalis
[Vasopressin V2 receptor antagonists: pharmacological properties and clinical implications].
December 2005, Harefuah,
J G Verbalis
Do vasopressin V2 receptor antagonists benefit cirrhotics with refractory ascites?
November 2015, World journal of gastroenterology,
J G Verbalis
Vasopressin V2-receptor antagonists in patients with cirrhosis, ascites and hyponatremia.
May 2012, Therapeutic advances in gastroenterology,
J G Verbalis
Synthesis and characterization of orally active nonpeptide vasopressin V2 receptor antagonists.
April 1999, Chemical & pharmaceutical bulletin,
J G Verbalis
V2 vasopressin receptor mutations.
January 2020, Vitamins and hormones,
J G Verbalis
V2-vasopressin receptor antagonists-mechanism of effect and clinical implications in hyponatraemia.
November 1999, Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association,
J G Verbalis
Vasopressin V2 receptor antagonists for the syndrome of inappropriate antidiuretic hormone secretion.
January 2024, International urology and nephrology,
J G Verbalis
The role of V2 vasopressin antagonists in hyponatremia.
August 2001, Cardiovascular research,
J G Verbalis
Vasopressin V2 (SR121463A) and V1a (SR49059) receptor antagonists both inhibit desmopressin vasorelaxing activity.
November 1999, European journal of pharmacology,
Copied contents to your clipboard!