Lemmens-Gruber R, Kamyar M
Department of Pharmacology and Toxicology, University of Vienna, 1090 Vienna, Austria.
Cell Mol Life Sci. 2006 Aug;63(15):1766-79. doi: 10.1007/s00018-006-6054-2.
Effects of vasopressin via V1a- and V2-receptors are closely implicated in a variety of water-retaining diseases and cardiovascular diseases, including heart failure, hyponatraemia, hypertension, renal diseases, syndrome of inappropriate antidiuretic hormone secretion, cirrhosis and ocular hypertension. As vasopressin receptors are found in many different tissues, vasopressin antagonists may benefit the treatment of disorders such as cerebral ischaemia and stroke, Raynaud's disease, dysmenorrhoea and tocolytic treatment. V1b selective vasopressin antagonists are discussed in terms of their usefulness in the treatment of emotional and psychiatric disorders. The vaptans are vasopressin receptor antagonists with V1a (relcovaptan) or V2 (tolvaptan, lixivaptan) selectivity or non-selective activity (conivaptan) which may be advantageous in some disorders. The V1a/V2 non-selective vasopressin antagonist conivaptan is the first vaptan which is approved by the FDA for the treatment of euvolaemic hyponatraemia.
血管加压素通过V1a和V2受体产生的作用与多种水潴留性疾病和心血管疾病密切相关，包括心力衰竭、低钠血症、高血压、肾脏疾病、抗利尿激素分泌不当综合征、肝硬化和高眼压症。由于血管加压素受体存在于许多不同组织中，血管加压素拮抗剂可能有益于治疗诸如脑缺血和中风、雷诺病、痛经以及安胎治疗等疾病。V1b选择性血管加压素拮抗剂在治疗情绪和精神障碍方面的效用也在讨论之中。血管加压素受体拮抗剂（vaptans）具有对V1a（瑞考伐坦）或V2（托伐普坦、利伐普坦）的选择性或非选择性活性（考尼伐坦），在某些疾病中可能具有优势。V1a/V2非选择性血管加压素拮抗剂考尼伐坦是首个获美国食品药品监督管理局批准用于治疗等容性低钠血症的血管加压素受体拮抗剂。
