CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors.

  title={CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors.},
  author={D. Schulz and R. Mansbach and J. Sprouse and J. Braselton and J. Collins and M. Corman and A. Dunaiskis and S. Faraci and Anne W. Schmidt and T. Seeger and P. Seymour and F. Tingley and E. Winston and Y. Chen and J. Heym},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  volume={93 19},
  • D. Schulz, R. Mansbach, +12 authors J. Heym
  • Published 1996
  • Chemistry, Medicine
  • Proceedings of the National Academy of Sciences of the United States of America
Here we describe the properties of CP-154,526, a potent and selective nonpeptide antagonist of corticotropin (ACTH) releasing factor (CRF) receptors. CP-154,526 binds with high affinity to CRF receptors (Ki < 10 nM) and blocks CRF-stimulated adenylate cyclase activity in membranes prepared from rat cortex and pituitary. Systemically administered CP-154,526 antagonizes the stimulatory effects of exogenous CRF on plasma ACTH, locus coeruleus neuronal firing and startle response amplitude… Expand
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Chapter 1 Recent Advances in Corticotropin-Releasing Factor Receptor Antagonists
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