Campbell W B, Pettinger W A
J Pharmacol Exp Ther. 1976 Aug;198(2):450-6.
Des-Asp angiotensin II (des-Asp AII) is a naturally occurring heptapeptide metabolite of angiotensin II (AII) which is formed by the enzymatic action of aminopeptidase A. Angiotensin II and des-Asp AII were infused into unanesthetized rats while direct mean arterial pressure, serum aldosterone and serum corticosterone were measured. Both AII and des-Asp AII caused a dose-related increase in serum aldosterone with a significant increase occurring with a dose as low as 1 ng/min. This effect was blocked by pretreatment with 1-Sar-8-Ala-angiotensin II, a competitive inhibitor of AII; however, the inhibitor was more effective in blocking the effects of AII (101%) than of des-Asp AII (82%). Both angiotensins induced a dose-related increase in serum corticosterone and mean arterial pressure. Des-Asp AII was however only 1/10 as potent as AII in elevating mean arterial pressure. 1-Sar-8-Ala-AII was also effective in inhibiting the pressor effects of AII and des-Asp AII. These data illustrate a high degree of organ specificity or selectivity for des-Asp AII and a low specificity for AII. Aminopeptidase A and leucine aminopeptidase were identified in the adrenal cortex and medulla in large amounts. Des-Asp AII may thus be formed from AII locally in the adrenal gland prior to exerting its action at that site.
脱天冬氨酸血管紧张素II(des - Asp AII)是血管紧张素II(AII)的一种天然存在的七肽代谢产物,由氨肽酶A的酶促作用形成。在未麻醉的大鼠中输注血管紧张素II和脱天冬氨酸血管紧张素II,同时测量直接平均动脉压、血清醛固酮和血清皮质酮。AII和des - Asp AII均导致血清醛固酮呈剂量相关增加,低至1 ng/min的剂量时就出现显著增加。这种作用被AII的竞争性抑制剂1 - Sar - 8 - Ala - 血管紧张素II预处理所阻断;然而,该抑制剂在阻断AII的作用(101%)方面比des - Asp AII(82%)更有效。两种血管紧张素均诱导血清皮质酮和平均动脉压呈剂量相关增加。然而,des - Asp AII在升高平均动脉压方面的效力仅为AII的1/10。1 - Sar - 8 - Ala - AII在抑制AII和des - Asp AII的升压作用方面也有效。这些数据说明了des - Asp AII具有高度的器官特异性或选择性,而AII的特异性较低。在肾上腺皮质和髓质中大量鉴定出氨肽酶A和亮氨酸氨肽酶。因此,des - Asp AII可能在肾上腺局部由AII形成,然后在该部位发挥其作用。