Antidepressant-like effects of CP-154,526, a selective CRF1 receptor antagonist
Abstract
The effects of CP-154,526 (butyl-ethyl-[2,5-dimethyl-7-(2,4,6 -trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-amine), a selective corticotropin releasing factor (CRF1) receptor antagonist, were examined in the learned helplessness procedure, a putative model of depression with documented sensitivity to diverse classes of antidepressant drugs. Rats were exposed to a series of inescapable foot shocks on three consecutive days and tested in a shock-escape procedure on the fourth day. Animals exposed to 'helplessness' training performed poorly in the shock-escape test compared with control animals not receiving inescapable shocks. CP-154,526 (10-32 mg/kg, intraperitoneally) dose-dependently reversed the escape deficit when administered 60 min prior to the test session, but had no effect on the performance of control rats not receiving prior exposure to inescapable stress. In comparison, the tricyclic antidepressant imipramine (17.8 mg/kg) reversed the escape deficit after repeated, but not acute, administration. These data support evidence implicating stress systems in the pathophysiology of depression, and suggest potential efficacy of small-molecule CRF receptor antagonists in the treatment of affective disorders.
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CRF receptor antagonists could prevent learned helplessness because behavioral changes induced by IL-1 occur through central CRF secretion.
“CRF receptor antagonists could prevent learned helplessness[62] because the behavioral changes induced by IL-1 occur through central CRF secretion.”
From Neuroinflammation and cytokine abnormality in major depression: cause or consequence in that illness? (2016) · cites this paper as [62]
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- Authors
- Mansbach, R. S., Brooks, E. N., & Chen, Y. L.
- Affiliations
- Pfizer (United States) (US)
- Corresponding author
- Mansbach, Robert S
- Venue
- European Journal of Pharmacology
- Publisher
- Elsevier BV
- Published
- 1997-03
- Volume
- 323
- Issue
- 1
- Pages
- 21-26
- ISSN
- 0014-2999 (ISSN-L)
- OpenAlex
- W2079718339
- Cited by
- 195
- References
- 33
- Citations by year
- 2026: 2 · 2023: 1 · 2022: 1 · 2021: 2 · 2020: 1 · 2019: 7 · 2018: 1 · 2017: 5 · 2016: 2 · 2015: 2 · 2014: 2 · 2013: 3 · 2012: 7
- FWCI
- 9.04
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Neuroscience › Behavioral Neuroscience › Stress Responses and Cortisol
- Health Sciences › Medicine › Pharmacology › Treatment of Major Depression
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Keywords
- CP-154,526, CRF1 receptor antagonist, corticotropin-releasing factor, antidepressant-like effects, learned helplessness, depression, inescapable footshock, stress system, imipramine, pyrrolo[2,3-d]pyrimidine
- MeSH terms
- Analysis of Variance, Animals, Antidepressive Agents, Tricyclic, Depression, Disease Models, Animal, Helplessness, Learned, Imipramine, Injections, Intraperitoneal, Male, Pyrimidines, Pyrroles, Rats, Sprague-Dawley, Receptors, Corticotropin-Releasing Hormone, Rats
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