Non-peptide arginine-vasopressin antagonists: the vaptans
Non-peptide arginine-vasopressin antagonists: the vaptans
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DOI：
10.1016/s0140-6736(08)60695-9
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发表时间：
2008-05-10
期刊：
影响因子：
168.9
通讯作者：
Vassart, Gilbert
中科院分区：
文献类型：
--
作者：
Decaux, Guy;Soupart, Alain;Vassart, Gilbert
精氨酸加压素是一种在循环和水稳态中发挥重要作用的激素。三种精氨酸加压素受体亚型 - V1a、V1b 和 V2 - 均属于视紫红质样 G 蛋白偶联受体大家族。 vaptans 是正在开发的口服和静脉注射活性非肽加压素受体拮抗剂。 Relcovaptan 是一种选择性 V1a 受体拮抗剂，在治疗雷诺氏病、痛经和安胎方面已显示出初步积极效果。 SSR-149415 是一种选择性 V1b 受体拮抗剂，可能对精神疾病的治疗产生有益作用。 V2 受体拮抗剂 - 莫扎伐普坦、利西伐普坦、沙伐普坦和托伐普坦 - 诱导高度低渗利尿，而不会显着影响电解质的排泄（与利尿剂的作用相反）。这些药物对于治疗血容量正常和血容量过多的低钠血症均有效。 Conivaptan 是一种 V1a/V2 非选择性加压素受体拮抗剂，已被美国食品和药物管理局批准用于静脉输注，用于院内治疗正常血容量或高血容量低钠血症。
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, dysmenorrhorea, 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.