Hata T, Ogihara T, Mikami H, Nakamaru M, Mandai T, Kumahara Y
Eur J Clin Pharmacol. 1980 Oct;18(4):295-9. doi: 10.1007/BF00561385.
Two angiotensin II analogues (AIIA), 1-sarcosine, 8-isoleucine angiotensin II ([Sar, Ile]-AII) and 1-sarcosine, 8-alanine angiotensin II ([Sar, Ala]-AII), were infused in six normal volunteers on high, regular and low sodium diets. The agonist and antagonist activities of these AIIA on blood pressure (BP), plasma aldosterone concentration (PAC), creatinine clearance and plasma renin activity were examined. Both AIIA had agonistic pressor activities in subjects on high and regular sodium diets, [Sar, Ile]-AII being more potent than [Sar, Ala]-AII. Both AIIA caused similar elevation of PAC in subjects on high and regular sodium diets, and an equally fall in PAC in subjects on a low sodium diet. Both AIIA strongly antagonized the rise in BP, the increase in PAC and the reduction of Ccr induced by AII administration in subjects on all three sodium diets. The results indicate that both AIIA can be used to examine the activity of the renin-angiotensin system in patients with hypertension, and they also suggest that AII interaction with its receptors differs in different target tissues.
将两种血管紧张素II类似物(AIIA),即1-肌氨酸、8-异亮氨酸血管紧张素II([Sar, Ile]-AII)和1-肌氨酸、8-丙氨酸血管紧张素II([Sar, Ala]-AII),分别输注给6名食用高钠、常规钠和低钠饮食的正常志愿者。检测了这些AIIA对血压(BP)、血浆醛固酮浓度(PAC)、肌酐清除率和血浆肾素活性的激动剂和拮抗剂活性。在食用高钠和常规钠饮食的受试者中,两种AIIA均具有升压激动活性,[Sar, Ile]-AII比[Sar, Ala]-AII更有效。在食用高钠和常规钠饮食的受试者中,两种AIIA均使PAC有相似程度的升高,而在食用低钠饮食的受试者中,两种AIIA使PAC同等程度地下降。在所有三种钠饮食的受试者中,两种AIIA均强烈拮抗由给予AII所诱导的血压升高、PAC增加和肌酐清除率降低。结果表明,两种AIIA均可用于检测高血压患者肾素-血管紧张素系统的活性,并且还提示AII与其受体在不同靶组织中的相互作用有所不同。