在多取代催产素中，结合了高催产活性以及可忽略不计的抗利尿和升压活性。

Combined high oxytocic with negligible antidiuretic and pressor activities in multisubstituted oxytocins.

作者信息

Stahl G L, Walter R

出版信息

J Med Chem. 1977 Apr;20(4):492-5. doi: 10.1021/jm00214a006.

Abstract

Oxytocin analogues which combine high oxytocic activities with negligible antidiuretic and pressor activities have been studied. [4-Threonine,7-glycine]oxytocin, [1-(L-2-hydroxy-3-mercaptopropionic acid),4-threonine,7-glycine]oxytocin, and [1-(L-2-hydroxy-3-mercaptopropionic acid)]oxytocin were found to possess the following specific biological activities respectively: rat uterotonic, 270 +/- 10, 337 +/- 23, 1542 +/- 0.4; rat antidiuretic, 0.002 +/- 0.0008, 0.048 +/- 0.005, 40.3 +/- 2.4. The results are analyzed from a conformation-activity viewpoint in a continued attempt to evaluate the scope and limitations of this approach in comparison to structure-activity studies.

摘要

人们已对兼具高效催产活性且抗利尿和升压活性可忽略不计的催产素类似物展开了研究。已发现[4-苏氨酸，7-甘氨酸]催产素、[1-(L-2-羟基-3-巯基丙酸)，4-苏氨酸，7-甘氨酸]催产素和[1-(L-2-羟基-3-巯基丙酸)]催产素分别具有以下特定生物活性：大鼠子宫收缩活性，270±10、337±23、1542±0.4；大鼠抗利尿活性，0.002±0.0008、0.048±0.005、40.3±2.4。从构象-活性的角度对结果进行了分析，持续尝试评估该方法相较于构效关系研究的适用范围和局限性。