Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.

@article{Frantz2010SubtletyOT,
  title={Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.},
  author={Marie-C{\'e}line Frantz and Jordi Rodrigo and Laure Boudier and Thierry Durroux and Bernard Mouillac and Marcel Hibert},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 4},
  pages={1546-62}
}
Very few nonpeptide oxytocin agonists have currently been reported, and none of them seem suitable for the in vivo investigation of the oxytocin mediated functions. In an attempt to rationalize the design of better tools, we have systematically studied the structural determinants of the affinity and efficacy of representative ligands of the V(1a), V(2), and OT receptor subtypes. Despite apparently obvious similarity between the ligand structures on one hand, and between the receptor subtypes on… CONTINUE READING