Glodny Bernhard, Pauli Guido F
Department of Radiology, Innsbruck Medical University, Austria.
Hypertens Res. 2006 Jul;29(7):533-44. doi: 10.1291/hypres.29.533.
The objective of this study was to further characterize the antihypertensive properties of medullipin and a second hormone designated angiolysin physiologically. Angiolysin and medullipin were tested in coronary and aortic rings from cows, sheep, pigs, mice and rats. In vivo animal experiments were performed using spontaneously hypertensive rats. Medullipin was successfully separated from another antihypertensive agent at the polar end of the polarity continuum. It is an extremely potent vasodilator. With the methods available today, it is not possible to make a galenical preparation of medullipin for in vivo analysis. The newly discovered antihypertensive agent is another extremely potent vasodilator, even stronger than medullipin, and was therefore named angiolysin. The vasodilatory activity of both medullipin and angiolysin persisted for hours, on rat and mouse aortae, and on the coronary arteries of pigs, cows and sheep. Both substances exerted their effects even in animal rings that were precontracted with 100 mmol/l K+. Angiolysin reduced the resting tension in blood vessels from mice and rats even without precontraction. A single injection of angiolysin resulted in a dose-dependent reduction of blood pressure, independent of the initial blood pressure, even to zero if the dosage was sufficient. The effect persisted for several hours. In conclusion, both hormones are extremely potent vasodilators, and are expected to lead to paradigmatic changes in the treatment of hypertension. With regard to potency, only sodium nitroprusside is comparable, but the effects of medullipin and angiolysin persist for hours after a single injection.
本研究的目的是从生理学角度进一步表征髓质素和另一种名为血管溶素的激素的降压特性。在来自牛、羊、猪、小鼠和大鼠的冠状动脉环和主动脉环中对血管溶素和髓质素进行了测试。使用自发性高血压大鼠进行了体内动物实验。髓质素已成功地从极性连续体极性末端的另一种降压剂中分离出来。它是一种极其有效的血管扩张剂。就目前可用的方法而言,不可能制备用于体内分析的髓质素盖伦制剂。新发现的降压剂是另一种极其有效的血管扩张剂,甚至比髓质素更强,因此被命名为血管溶素。髓质素和血管溶素的血管舒张活性在大鼠和小鼠主动脉以及猪、牛和羊的冠状动脉上持续数小时。即使在预先用100 mmol/l K+预收缩的动物血管环中,这两种物质也能发挥作用。血管溶素即使在未预先收缩的情况下也能降低小鼠和大鼠血管的静息张力。单次注射血管溶素会导致血压剂量依赖性降低,与初始血压无关,如果剂量足够甚至可降至零。这种作用持续数小时。总之,这两种激素都是极其有效的血管扩张剂,有望在高血压治疗中引发范式性变化。就效力而言,只有硝普钠可与之相比,但髓质素和血管溶素的作用在单次注射后会持续数小时。