Department of Pharmacology, Vanderbilt University Medical Center, 1161 21 Ave, Medical Center North # B3214, Nashville, TN 37232-2372, USA.
Hypertension. 2012 Nov;60(5):1184-91. doi: 10.1161/HYPERTENSIONAHA.112.199026. Epub 2012 Sep 24.
Prostaglandin E(2) is a major prostanoid found in the kidney and vasculature contributing to the regulation of blood pressure. The prostaglandin E(2) receptor EP1 has been shown to contribute to hypertension by mediating angiotensin II-dependent vasoconstriction, although its precise role is incompletely characterized. Disruption of the EP1 receptor in C57BL/6J mice reduced the incidence of mortality during severe hypertension induced by uninephrectomy, deoxycorticosterone acetate, and angiotensin II. Mortality was dependent on all components of the model. Death was a result of aortic aneurysm rupture or occurred after development of anasarca, each of which was reduced in EP1-/- mice. Mean arterial pressure was increased in treated EP1+/+ and EP1-/- mice; however, this elevation was significantly lower in EP1-/- mice. Blood pressure reduction via administration of hydralazine phenocopied EP1-/- mice. Thus, reduction in blood pressure by disruption of EP1 reduced incidence of mortality and decreased organ damage, suggesting that EP1 receptor blockade may be a viable target for antihypertensive therapy.
前列腺素 E(2)是肾脏和血管中发现的一种主要的前列腺素,有助于调节血压。已经表明,前列腺素 E(2)受体 EP1 通过介导血管紧张素 II 依赖性血管收缩来导致高血压,尽管其确切作用尚未完全阐明。在 C57BL/6J 小鼠中破坏 EP1 受体可降低单侧肾切除、脱氧皮质酮醋酸盐和血管紧张素 II 诱导的严重高血压期间的死亡率。死亡率取决于模型的所有组成部分。死亡是由于主动脉瘤破裂或发生全身性水肿后导致的,而这两种情况在 EP1-/- 小鼠中均减少。在接受治疗的 EP1+/+ 和 EP1-/- 小鼠中,平均动脉压升高;然而,EP1-/- 小鼠中的这种升高明显较低。通过给予肼屈嗪降低血压可模拟 EP1-/- 小鼠的情况。因此,通过破坏 EP1 降低血压可降低死亡率和减少器官损伤,这表明 EP1 受体阻断可能是一种可行的抗高血压治疗靶点。