Linked Life Data

16713496

Source:http://linkedlifedata.com/resource/pubmed/id/16713496

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
2006-5-22
pubmed:abstractText
Hyponatremia is a frequent and symptomatic electrolyte disorder for which specific treatments have been lacking. Hyponatremia is attributable to nonosmotic vasopressin stimulation and continued increased fluid intake. In the past, peptidic derivatives of arginine vasopressin proved that blockade of vasopressin V-2 receptors served to improve hyponatremia, however, these antagonists had intrinsic agonistic activity, too. In the past decade, random screening of molecules uncovered nonpeptide, orally available vasopressin antagonists without agonistic properties. The agents show competitive binding to the vasopressin V-2 receptor at an affinity comparable with that of arginine vasopressin. Four antagonists have undergone extensive study. Three of these agents--lixivaptan or VPA 985; SR 121 463 B; tolvaptan or OPC 41,061--are specific V-2 antagonists whereas conivaptan or YM 087 is a V-1/V-2 mixed antagonist. In animal and clinical studies all of the agents were able to correct water retention and hyponatremia in a dose-dependent manner. There was no tachyphylaxis, even when the agents were given over many weeks. It is expected that the clinical use of the agents will lead to a major improvement in the treatment of hyponatremia.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0270-9295
pubmed:author
pubmed:issnType
Print
pubmed:volume
26
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
234-43
pubmed:meshHeading
pubmed:year
2006
pubmed:articleTitle
Vaptans and the treatment of water-retaining disorders.
pubmed:affiliation
Nephrologie, Medizinische Klinik III, Universitätsklinikum C.G. Carus, Dresden, Germany.
pubmed:publicationType
Journal Article, Review