Behm David J, Harrison Stephen M, Ao Zhaohui, Maniscalco Kristeen, Pickering Susan J, Grau Evelyn V, Woods Tina N, Coatney Robert W, Doe Christopher P A, Willette Robert N, Johns Douglas G, Douglas Stephen A
Department of Vascular Biology, Cardiovascular and Urogenital Diseases Center of Excellence for Drug Discovery, GlaxoSmithKline, King of Prussia, PA 19406-0939, USA.
Br J Pharmacol. 2003 May;139(2):464-72. doi: 10.1038/sj.bjp.0705254.
1 Urotensin-II (U-II) is among the most potent mammalian vasoconstrictors identified and may play a role in the aetiology of essential hypertension. Currently, only one mouse U-II receptor (UT) gene has been cloned. It is postulated that this protein is solely responsible for mediating U-II-induced vasoconstriction. 2 This hypothesis has been investigated in the present study, which assessed basal haemodynamics and vascular reactivity to hU-II in wild-type (UT((+/+))) and UT receptor knockout (UT((-/-))) mice. 3 Basal left ventricular end-diastolic and end-systolic volumes/pressures, stroke volumes, mean arterial blood pressures, heart rates, cardiac outputs and ejection fractions in UT((+/+)) mice and in UT((-/-)) mice were similar. 4 Relative to UT((+/+)) mouse isolated thoracic aorta, where hU-II was a potent spasmogen (pEC(50)=8.26+/-0.08) that evoked relatively little vasoconstriction (17+/-2% 60 mM KCl), vessels isolated from UT((-/-)) mice did not respond to hU-II. However, in contrast, the superior mesenteric artery isolated from both the genotypes did not contract in the presence of hU-II. Reactivity to unrelated vasoconstrictors (phenylephrine, endothelin-1, KCl) and endothelium-dependent/independent vasodilator agents (carbachol, sodium nitroprusside) was similar in the aorta and superior mesenteric arteries isolated from both the genotypes. 5 The present study is the first to directly link hU-II-induced vasoconstriction with the UT receptor. Deletion of the UT receptor gene results in loss of hU-II contractile action with no 'nonspecific' alterations in vascular reactivity. However, as might be predicted based on the limited contractile efficacy recorded in vitro, the contribution that hU-II and its receptor make to basal systemic haemodynamics appears to be negligible in this species.
1 尾加压素II(U-II)是已发现的最有效的哺乳动物血管收缩剂之一,可能在原发性高血压的病因学中起作用。目前,仅克隆了一个小鼠U-II受体(UT)基因。据推测,该蛋白是介导U-II诱导的血管收缩的唯一原因。2 本研究对这一假设进行了调查,评估了野生型(UT((+/+)))和UT受体敲除(UT((-/-)))小鼠的基础血流动力学以及对人U-II的血管反应性。3 UT((+/+))小鼠和UT((-/-))小鼠的基础左心室舒张末期和收缩末期容积/压力、每搏量、平均动脉血压、心率、心输出量和射血分数相似。4 相对于UT((+/+))小鼠分离的胸主动脉,人U-II在其中是一种有效的致痉剂(pEC(50)=8.26±0.08),可引起相对较小的血管收缩(17±2% 60 mM氯化钾),从UT((-/-))小鼠分离的血管对人U-II无反应。然而,相比之下,从两种基因型分离的肠系膜上动脉在人U-II存在时均不收缩。从两种基因型分离的主动脉和肠系膜上动脉对无关血管收缩剂(去氧肾上腺素、内皮素-1、氯化钾)以及内皮依赖性/非依赖性血管舒张剂(卡巴胆碱、硝普钠)的反应性相似。5 本研究首次直接将人U-II诱导的血管收缩与UT受体联系起来。UT受体基因的缺失导致人U-II收缩作用丧失,且血管反应性无“非特异性”改变。然而,正如基于体外记录的有限收缩效力所预测的那样,人U-II及其受体对基础全身血流动力学的贡献在该物种中似乎可以忽略不计。