Non-peptide arginine-vasopressin antagonists: the vaptans
作者： Guy Decaux , Alain Soupart , Gilbert Vassart
DOI: 10.1016/S0140-6736(08)60695-9
关键词: Relcovaptan 、 Pharmacology 、 Internal medicine 、 Lixivaptan 、 Satavaptan 、 Vasopressin Antagonists 、 Conivaptan 、 Antagonist 、 Vasopressin 、 Antidiuretic Hormone Receptor Antagonists 、 Medicine 、 Endocrinology
摘要: Arginine-vasopressin is a hormone that plays an important part in circulatory and water homoeostasis. The three arginine-vasopressin-receptor subtypes--V1a, V1b, V2--all belong to the large rhodopsin-like G-protein-coupled receptor family. vaptans are orally intravenously active non-peptide vasopressin antagonists development. Relcovaptan selective V1a-receptor antagonist, which has shown initial positive results treatment of Raynaud's disease, dysmenorrhoea, tocolysis. SSR-149415 V1b-receptor could have beneficial effects psychiatric disorders. V2-receptor antagonists--mozavaptan, lixivaptan, satavaptan, tolvaptan--induce highly hypotonic diuresis without substantially affecting excretion electrolytes (by contrast with diuretics). These drugs all effective euvolaemic hypervolaemic hyponatraemia. Conivaptan V1a/V2 non-selective vasopressin-receptor antagonist been approved by US Food Drug Administration as intravenous infusion for inhospital or
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