The Macrocyclic Peptide Natural Product CJ-15,208 Is Orally Active and Prevents Reinstatement of Extinguished Cocaine-Seeking Behavior
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Issue Date
2013-01-17Author
Aldrich, Jane V.
Senadheera, Sanjeewa N.
Ross, Nicolette C.
Ganno, Michelle L.
Eans, Shainnel O.
McLaughlin, Jay P.
Publisher
Journal of Natural Products
Type
Article
Article Version
Scholarly/refereed, publisher version
Rights
Copyright © 2013 The American Chemical Society and American Society of Pharmacognosy
Metadata
Show full item recordAbstract
The macrocyclic tetrapeptide natural product CJ-15,208 (cyclo[Phe-d-Pro-Phe-Trp]) exhibited both dose-dependent antinociception and kappa opioid receptor (KOR) antagonist activity after oral administration. CJ-15,208 antagonized a centrally administered KOR selective agonist, providing strong evidence it crosses the blood–brain barrier to reach KOR in the CNS. Orally administered CJ-15,208 also prevented both cocaine- and stress-induced reinstatement of extinguished cocaine-seeking behavior in the conditioned place preference assay in a time- and dose-dependent manner. Thus, CJ-15,208 is a promising lead compound with a unique activity profile for potential development, particularly as a therapeutic to prevent relapse to drug-seeking behavior in abstinent subjects.
Collections
- Pharmacy Scholarly Works [293]
Citation
Aldrich, Jane V., Sanjeewa N. Senadheera, Nicolette C. Ross, Michelle L. Ganno, Shainnel O. Eans, and Jay P. Mclaughlin. "The Macrocyclic Peptide Natural Product CJ-15,208 Is Orally Active and Prevents Reinstatement of Extinguished Cocaine-Seeking Behavior." Journal of Natural Products 76.3 (2013): 433-38.
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