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

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Abstract
Oxytocin analogues which combine high oxytocic activities with negligible antidiuretic and pressor activities were 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 possessed the following specific biological activities, respectively: rat uterotonic, 270 .+-. 10, 337 .+-. 23, 1542 .+-. 18; avian [chicken] vasodepressor, 8.6 .+-. 0.2, 50 .+-. 4, 1778 .+-. 25; rat pressor, mixed depressor/pressor, mixed depressor/pressor, 23.7 .+-. 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.