Watanabe T X, Sokabe H, Honda I, Sakakibara S, Nakayama T
Jpn J Pharmacol. 1977 Feb;27(1):137-44. doi: 10.1254/jjp.27.137.
Specific pressor activity of Asp1-Val5-antiotensins I and II was determined by a 4-point assay in rats against various synthetic angiotensins. Specific pressor activity of various angiotensins was also obtained from the dose-blood pressure-response (DR) curve, using a single angiotensin sample per rat. Comparison of two values showed that two angiotensins interacted in the 4-point assay, yielding a potentiation factor of 0.465-1.373. Therefore, specific pressor activity from DR curve is more reliable, because two angiotensins are not able to interact. Potency ratio on a molar basis of Asp1-IIe5-angiotensin I, Asp1-Val5-angiotensins I and II, Asn1-Val5-angiotensin II (Ciba Lot-094691), and Asp1-Val5-Ser9-angiotensin I against Asp1-IIe5-angiotensin II were 0.76, 0.91, 2.02, 0.50, and 1.39, respectively. Asp1-Val5-angiotensin II had twice the pressor activity of Asp1-IIe5-angiotensin II. Lyophylized Asp1-IIe5-angiotensins I and II kept desiccated at --20 degrees C, were stable for 27 months. Solutions of 100, 10, and 0.8 microng/ml were stable for 12, 8, and 6 months at--20 degrees C, respectively.
通过在大鼠身上针对各种合成血管紧张素的四点测定法,确定了天冬氨酸1-缬氨酸5-血管紧张素I和II的比升压活性。还使用每只大鼠的单个血管紧张素样本,从剂量-血压反应(DR)曲线获得了各种血管紧张素的比升压活性。两种值的比较表明,在四点测定法中两种血管紧张素相互作用,产生的增效因子为0.465-1.373。因此,来自DR曲线的比升压活性更可靠,因为两种血管紧张素无法相互作用。天冬氨酸1-异亮氨酸5-血管紧张素I、天冬氨酸1-缬氨酸5-血管紧张素I和II、天冬酰胺1-缬氨酸5-血管紧张素II(汽巴批号-094691)以及天冬氨酸1-缬氨酸5-丝氨酸9-血管紧张素I相对于天冬氨酸1-异亮氨酸5-血管紧张素II的摩尔效价比分别为0.76、0.91、2.02、0.50和1.39。天冬氨酸1-缬氨酸5-血管紧张素II的升压活性是天冬氨酸1-异亮氨酸5-血管紧张素II的两倍。冻干的天冬氨酸1-异亮氨酸5-血管紧张素I和II在-20℃下干燥保存,27个月内稳定。100、10和0.8微克/毫升的溶液在-20℃下分别可稳定12、8和6个月。