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Proc Natl Acad Sci U S A. 1996 Sep 17;93(19):10477-82.

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

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1
Department of Neuroscience, Pfizer Central Research, Groton, CT 06340, USA.

Abstract

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. Potential anxiolytic activity of CP-154,526 was revealed in a fearpotentiated startle paradigm. These data are presented in the context of clinical findings, which suggest that CRF is hypersecreted in certain pathological states. We propose that a CRF antagonist such as CP-154,526 could affirm the role of CRF in certain psychiatric diseases and may be of significant value in the treatment of these disorders.

PMID:
8816826
PMCID:
PMC38410
[Indexed for MEDLINE]
Free PMC Article
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