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

@article{Schulz1996CP154526AP,
  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},
  year={1996},
  volume={93 19},
  pages={
          10477-82
        }
}
  • 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
The pharmacology of CP-154,526, a non-peptide antagonist of the CRH1 receptor: a review.
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The present findings suggest that chronic administration of CP-154, 526 produces anxiolytic-like effects but no evidence of adrenal insufficiency. Expand
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Data support the hypothesis that the CRF(2) receptor mediates the appetite suppression induced by CRF and suggest that theCRF( 2) receptor could mediate the stress-like behaviors that accompany CRF-induced appetite suppression. Expand
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A role for CRF binding sites in co-ordinating stress reactivity, emotionality and energy balance over the life-span of the organism is supported. Expand
Chapter 1 Recent Advances in Corticotropin-Releasing Factor Receptor Antagonists
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The authors provide a detailed description of the endogenous receptors and peptide ligands in this family as well as a review of the current non-peptide small molecule antagonists that may yield the first proof of concept for this system in disease. Expand
The corticotropin-releasing factor receptor 1 antagonist CP-154,526 reverses stress-induced learning deficits in mice
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It is demonstrated that learning impairment after acute stress was antagonized by CP-154,526 pretreatment, and the CP- 154,526-induced enhancements in fear conditioning and PPF could be prevented by the selective CaMKII inhibitor KN-62. Expand
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