三脯氨酰和五肌氨酰血管紧张素II的选择性药理作用
Selective pharmacological effects of triprolyl and pentasarcosyl angiotensin II.
作者信息
Mikami H, Ogihara T, Katahira K, Imai N, Kumahara Y, Bumpus F M, Khosla M C
出版信息
J Cardiovasc Pharmacol. 1987 Feb;9(2):242-5. doi: 10.1097/00005344-198702000-00019.
Among the various biological effects of angiotensin II (AII), both pressor activity and aldosterone stimulation appear to be mediated by functionally different receptors. With this in mind, we compared pressor and aldosterone-stimulating activities of AII with those of triprolyl [(Pro)3] AII and pentasarcosyl [(Sar)5] AII. In conscious male Wistar rats (Pro)3 AII and (Sar)5 AII produced 48 and 46% of the pressor activity of AII. After intravenous infusion (conscious unrestrained rats, 125 pmol/kg/min for 30 min), plasma aldosterone concentrations were not significantly different from those of control rats which were infused with saline. However, when the rats were infused with AII (125 pmol/kg/min for 30 min), plasma aldosterone concentrations increased significantly (1,306 +/- 80 pg/ml). This study indicates that (Pro)3 AII and (Sar)5 AII may prove to be useful tools to elucidate biological actions of AII.
在血管紧张素II（AII）的各种生物学效应中，其升压活性和醛固酮刺激作用似乎是由功能不同的受体介导的。考虑到这一点，我们比较了AII与三脯氨酰[（Pro）3] AII和五肌氨酰[（Sar）5] AII的升压活性和醛固酮刺激活性。在清醒雄性Wistar大鼠中，（Pro）3 AII和（Sar）5 AII产生的升压活性分别为AII的48%和46%。静脉输注后（清醒不受约束的大鼠，125 pmol/kg/分钟，持续30分钟），血浆醛固酮浓度与输注生理盐水的对照大鼠相比无显著差异。然而，当大鼠输注AII（125 pmol/kg/分钟，持续30分钟）时，血浆醛固酮浓度显著升高（1306±80 pg/ml）。本研究表明，（Pro）3 AII和（Sar）5 AII可能被证明是阐明AII生物学作用的有用工具。
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