Combined high oxytocic with negligible antidiuretic and pressor activities in multisubstituted oxytocins.
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.
D000818:Animals; D001794:Blood Pressure / Q000187:drug effects*; D002645:Chickens; D004231:Diuresis / Q000187:drug effects*; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D010120:Oxytocics / Q000138:chemical synthesis*; D010121:Oxytocin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D013997:Time Factors; D014599:Uterus / Q000187:drug effects
D010120:Oxytocics; D010121:Oxytocin