Effect of threonine in position 4 in oxytocin and vasotocin analogs on the time course of uterotonic response.
The substitution of glutamine by threonine in position 4 of oxytocin, deamino-oxytocin, deamino-1-carba-oxytocin, and deamino-6-carba-oxytocin was found to increase the elimination rate of all analogs examined from the uterine receptor compartment in rat. However, this substitution was without any effect on the time course of uterotonic response in the case of vasotocin and deamino-vasotocin. These results suggest that the topological relationships of the 4 and 8 positions may show an important effect on elimination rate of oxytocin and vasotocin analogs from the rat uterine compartment.
D000818:Animals; D005260:Female; D010121:Oxytocin / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D013912:Threonine / Q000494:pharmacology*; D014590:Uterine Contraction / Q000187:drug effects*; D014668:Vasotocin / Q000031:analogs & derivatives* / Q000494:pharmacology
D013912:Threonine; D010121:Oxytocin; D014668:Vasotocin