CP-154,526
CP-154,526 is a potent and selective antagonist of the corticotropin releasing hormone receptor 1 developed by Pfizer.[1]
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N-butyl-N-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[3,2-e]pyrimidin-4-amine | |
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| C23H32N4 | |
| Molar mass | 364.52698 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
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CP-154,526 is under investigation for the potential treatment of alcoholism.[2][3]
References
- Schulz DW, Mansbach RS, Sprouse J, Braselton JP, Collins J, Corman M, Dunaiskis A, Faraci S, Schmidt AW, Seeger T, Seymour P, Tingley FD, Winston EN, Chen YL, Heym J (September 1996). "CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors". Proceedings of the National Academy of Sciences of the United States of America. 93 (19): 10477–82. Bibcode:1996PNAS...9310477S. doi:10.1073/pnas.93.19.10477. PMC 38410. PMID 8816826.
- "Drug Has Potential To Prevent Alcoholics From Relapsing". Science News. ScienceDaily. 2008-08-02. Retrieved 2008-08-09.
- Pastor R, McKinnon CS, Scibelli AC, Burkhart-Kasch S, Reed C, Ryabinin AE, Coste SC, Stenzel-Poore MP, Phillips TJ (July 2008). "Corticotropin-releasing factor-1 receptor involvement in behavioral neuroadaptation to ethanol: a urocortin1-independent mechanism". Proceedings of the National Academy of Sciences of the United States of America. 105 (26): 9070–5. Bibcode:2008PNAS..105.9070P. doi:10.1073/pnas.0710181105. PMC 2449366. PMID 18591672.
Further reading
- Seymour PA, Schmidt AW, Schulz DW (2006). "The pharmacology of CP-154,526, a non-peptide antagonist of the CRH1 receptor: a review". CNS Drug Reviews. 9 (1): 57–96. doi:10.1111/j.1527-3458.2003.tb00244.x. PMC 6741649. PMID 12595912.
- Navarro-Zaragoza J, Núñez C, Laorden ML, Milanés MV (May 2010). "Effects of corticotropin-releasing factor receptor-1 antagonists on the brain stress system responses to morphine withdrawal". Molecular Pharmacology. 77 (5): 864–73. doi:10.1124/mol.109.062463. PMID 20159948.
- Kobayashi T, Kiyokawa Y, Takeuchi Y, Mori Y (September 2011). "Pretreatment with CP-154526 blocks the modifying effects of alarm pheromone on components of sexual behavior in male, but not in female, rats". Chemical Senses. 36 (7): 623–32. doi:10.1093/chemse/bjr017. PMID 21502338.
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