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The Macrocyclic Peptide Natural Product CJ-15,208 Is Orally Active and Prevents Reinstatement of Extinguished Cocaine-Seeking Behavior
Aldrich, Jane V. Senadheera, Sanjeewa N. Ross, Nicolette C. Ganno, Michelle L. Eans, Shainnel O. McLaughlin, Jay P.
Aldrich, Jane V.
Senadheera, Sanjeewa N.
Ross, Nicolette C.
Ganno, Michelle L.
Eans, Shainnel O.
McLaughlin, Jay P.
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Abstract
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.
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2013-01-17
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Journal of Natural Products
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aldrich_macrocyclic.pdf
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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.