Non-peptide arginine-vasopressin antagonists: the vaptans
| Autor: | Gilbert Vassart, Guy Decaux, Alain Soupart |
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| Rok vydání: | 2008 |
| Předmět: |
Models
Molecular Receptors Vasopressin medicine.medical_specialty Vasopressin medicine.drug_class Relcovaptan Pharmacology Internal medicine Animals Humans Medicine Clinical Trials as Topic business.industry Contraindications Antidiuretic Agents Antagonist General Medicine Antidiuretic Hormone Receptor Antagonists Benzazepines Lixivaptan Arginine Vasopressin Satavaptan Endocrinology Conivaptan business Vasopressin Antagonists Hyponatremia medicine.drug |
| Zdroj: | The Lancet. 371:1624-1632 |
| ISSN: | 0140-6736 |
| DOI: | 10.1016/s0140-6736(08)60695-9 |
| Popis: | Arginine-vasopressin is a hormone that plays an important part in circulatory and water homoeostasis. The three arginine-vasopressin-receptor subtypes--V1a, V1b, and V2--all belong to the large rhodopsin-like G-protein-coupled receptor family. The vaptans are orally and intravenously active non-peptide vasopressin receptor antagonists that are in development. Relcovaptan is a selective V1a-receptor antagonist, which has shown initial positive results in the treatment of Raynaud's disease, dysmenorrhoea, and tocolysis. SSR-149415 is a selective V1b-receptor antagonist, which could have beneficial effects in the treatment of psychiatric disorders. V2-receptor antagonists--mozavaptan, lixivaptan, satavaptan, and tolvaptan--induce a highly hypotonic diuresis without substantially affecting the excretion of electrolytes (by contrast with the effects of diuretics). These drugs are all effective in the treatment of euvolaemic and hypervolaemic hyponatraemia. Conivaptan is a V1a/V2 non-selective vasopressin-receptor antagonist that has been approved by the US Food and Drug Administration as an intravenous infusion for the inhospital treatment of euvolaemic or hypervolaemic hyponatraemia. |
| Databáze: | OpenAIRE |
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