Loch David, Hoey Andrew, Brown Lindsay
Department of Physiology and Pharmacology, School of Biomedical Sciences, The University of Queensland, 4072, Australia.
Clin Exp Hypertens. 2006 Jul;28(5):475-88. doi: 10.1080/10641960600798754.
Omapatrilat, a vasopeptidase inhibitor, inhibits both neutral endopeptidase and angiotensin-converting enzyme with similar potency. The aim of this study was to investigate whether omapatrilat prevents or reverses cardiovascular remodeling and hypertension in deoxycorticosterone acetate (DOCA)-salt rats. Male Wistar rats (313 +/- 2 g, n = 114) were uninephrectomized (UNX) with or without further treatment with DOCA and 1% NaCl in the drinking water. Compared with UNX control rats, DOCA-salt rats developed hypertension, cardiovascular hypertrophy, perivascular and interstitial cardiac fibrosis and inflammation, endothelial dysfunction, and the prolongation of ventricular action potential duration within four weeks. The administration of omapatrilat (40 mg/kg/day po) for two weeks commencing two weeks after surgery attenuated the development of cardiovascular hypertrophy, inflammation, fibrosis, and ventricular action potential prolongation. In contrast, omapatrilat treatment did not lower systolic blood pressure nor improve endothelial dysfunction. This study concludes that the renin-angiotensin-aldosterone, natriuretic peptide, and bradykinin systems are directly involved in the pathogenesis of cardiovascular remodeling in the DOCA-salt model of hypertension in rats, which may be independent of their effects on blood pressure.
奥美帕替拉,一种血管肽酶抑制剂,以相似的效力抑制中性内肽酶和血管紧张素转换酶。本研究的目的是调查奥美帕替拉是否能预防或逆转醋酸脱氧皮质酮(DOCA)-盐大鼠的心血管重塑和高血压。雄性Wistar大鼠(313±2 g,n = 114)接受单侧肾切除术(UNX),并给予或不给予DOCA进一步处理,且饮用水中含有1% NaCl。与UNX对照大鼠相比,DOCA-盐大鼠在四周内出现高血压、心血管肥大、血管周围和间质心脏纤维化及炎症、内皮功能障碍以及心室动作电位时程延长。术后两周开始给予奥美帕替拉(40 mg/kg/天,口服)两周,可减轻心血管肥大、炎症、纤维化及心室动作电位延长的发展。相比之下,奥美帕替拉治疗并未降低收缩压,也未改善内皮功能障碍。本研究得出结论,肾素-血管紧张素-醛固酮、利钠肽和缓激肽系统直接参与大鼠DOCA-盐高血压模型中心血管重塑的发病机制,这可能与其对血压的影响无关。