Binding kinetics redefine the antagonist pharmacology of the corticotropin-releasing factor type 1 receptor.

@article{Fleck2012BindingKR,
  title={Binding kinetics redefine the antagonist pharmacology of the corticotropin-releasing factor type 1 receptor.},
  author={Beth A Fleck and Samuel R J Hoare and Rebecca R Pick and Margaret J. Bradbury and D. G. E. Grigoriadis},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2012},
  volume={341 2},
  pages={518-31}
}
Corticotropin-releasing factor (CRF) receptor antagonists are under preclinical and clinical investigation for stress-related disorders. In this study the impact of receptor-ligand binding kinetics on CRF₁ receptor antagonist pharmacology was investigated by measuring the association rate constant (k₁), dissociation rate constant (k₋₁), and kinetically derived affinity at 37°C. Three aspects of antagonist pharmacology were reevaluated: comparative binding activity of advanced compounds, in vivo… CONTINUE READING

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Influence of the N-terminus and the E2loop onto the binding kinetics of the antagonist mepyramine and the partial agonist phenoprodifen to H(1)R

  • HJ Wittmann, R Seifert, A Strasser
  • Biochem Pharmacol 82:1910-1918
  • 2011
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