Mechanisms of allosteric modulation at GABAB receptors by CGP7930 and GS39783: effects on affinities and efficacies of orthosteric ligands with distinct intrinsic properties.

@article{Urwyler2005MechanismsOA,
  title={Mechanisms of allosteric modulation at GABAB receptors by CGP7930 and GS39783: effects on affinities and efficacies of orthosteric ligands with distinct intrinsic properties.},
  author={Stephan Urwyler and Tina Gjoni and Jelena Koljati{\'c} and Delphine S. Dupuis},
  journal={Neuropharmacology},
  year={2005},
  volume={48 3},
  pages={343-53}
}
We determined the effects of the allosteric gamma-aminobutyric acid B receptor modulators CGP7930 and GS39783 on binding and function of orthosteric ligands with distinct intrinsic properties. In radioligand binding (saturation or displacement) experiments, the affinities of a number of competitive antagonists were decreased by the modulators, with no change in receptor number. The binding curves of the partial agonist CGP47656 comprised a high and a low affinity component; the affinity of the… CONTINUE READING