Receptor occupancy of nonpeptide corticotropin-releasing factor 1 antagonist DMP696: correlation with drug exposure and anxiolytic efficacy.

@article{Li2003ReceptorOO,
  title={Receptor occupancy of nonpeptide corticotropin-releasing factor 1 antagonist DMP696: correlation with drug exposure and anxiolytic efficacy.},
  author={Yu-Wen Li and Geraldine Hill and Harvey Wong and N. Kelly and K. Ward and Marie Pierdomenico and S. X. Ren and Paul J. Gilligan and Scott A. Grossman and George L Trainor and Rebecca Taub and John McElroy and Robert Zazcek},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2003},
  volume={305 1},
  pages={86-96}
}
4-(1,3-Dimethoxyprop-2-ylamine)-2,7-dimethyl-8-(2,4-dichlorophenyl)-pyrazolo[1,5-a]-1,3,5-triazine (DMP696) is a highly selective and potent, nonpeptide corticotropin-releasing factor 1 (CRF(1)) antagonist. In this study, we measured in vivo CRF(1) receptor occupancy of DMP696 by using ex vivo ligand binding and quantitative autoradiography and explored the relationship of receptor occupancy with plasma and brain exposure and behavioral efficacy. In vitro affinity (IC(50)) of DMP696 to brain… CONTINUE READING