Receptor Occupancy of Non-Peptide CRF1 Antagonist DMP696: Correlation with Drug Exposure and Anxiolytic Efficacy

نویسندگان

  • Yu-Wen Li
  • Geraldine Hill
  • Harvy Wong
  • Natasha Kelly
  • Kathryn Ward
  • Marie Pierdomenico
  • Shelly Ren
  • Paul Gilligan
  • Scott Grossman
  • George Trainor
  • Rebecca Taub
  • John McElroy
  • Robert Zazcek
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Receptor occupancy of nonpeptide corticotropin-releasing factor 1 antagonist DMP696: correlation with drug exposure and anxiolytic efficacy.

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 wi...

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تاریخ انتشار 2002