Wang J, Shi P
Shanghai Institute of Biochemistry, Academia Sinica.
Chin Med J (Engl). 1995 Apr;108(4):255-8.
Atriopeptin III (AP III) and its six analogues were synthesized by solid phase method and their diuretic and hypotensive activities were determined. Among these analogues, analogue [D-Ala-5, D-Arg-23] AP III was nearly 10 times as potent as AP III in diuretic activity while its hypotensive activity increased only 50% of that of AP III. Analogue des [Ser-15Gly-16Leu-17Gly-18Asn-20Ser-21] AP III was 15% as potent as AP III in diuretic activity, but it still maintained about 60% of the hypotensive activity of AP III. Meanwhile, we tried analogue [D-Ala-5, D-Agr-23] AP III for the treatment of hypertensive syndrome in pregnancy and obtained some good results.
采用固相法合成了心房肽Ⅲ（APⅢ）及其6种类似物，并测定了它们的利尿和降压活性。在这些类似物中，类似物[D-丙氨酸-5，D-精氨酸-23]APⅢ的利尿活性几乎是APⅢ的10倍，而其降压活性仅增加了APⅢ的50%。类似物去[丝氨酸-15甘氨酸-16亮氨酸-17甘氨酸-18天冬酰胺-20丝氨酸-21]APⅢ的利尿活性为APⅢ的15%，但仍保留了APⅢ约60%的降压活性。同时，我们尝试将类似物[D-丙氨酸-5，D-精氨酸-23]APⅢ用于治疗妊娠高血压综合征，并取得了一些良好的效果。
