Oxytocin receptor binding and uterotonic activity of carbetocin and its metabolites following enzymatic degradation.

@article{Engstrm1998OxytocinRB,
  title={Oxytocin receptor binding and uterotonic activity of carbetocin and its metabolites following enzymatic degradation.},
  author={Thomas Engstr{\o}m and Tomislav Barth and Per Melin and Hans Vilhardt},
  journal={European journal of pharmacology},
  year={1998},
  volume={355 2-3},
  pages={
          203-10
        }
}
Metabolites of the analogue 1-deamino-1-carba-2-tyrosine(O-methyl)-oxytocin (carbetocin) following incubation with a rat kidney homogenate were isolated and their pharmacodynamic properties investigated. Apart from the parent compound two metabolites were identified namely desGlyNH2-carbetocin (carbetocin metabolite I) and desLeuGlyNH2-carbetocin (carbetocin metabolite II). Both carbetocin, carbetocin metabolite I and carbetocin metabolite II displayed binding affinities to the myometrial… Expand
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TLDR
The curve-fit method was used to estimate the plasma half-lives of vasopressin and oxytocin analogs substituted in the 1, 1 and 6, and 8 positions, and three 8-substituted analogs of oxytocIn, including [8-ornithine]-oxytocin, were also long-acting. Expand
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