Tryptophan Substitution in CJ-15,208 (<i>cyclo</i>[Phe-D-Pro-Phe-Trp]) Introduces δ-Opioid Receptor Antagonism, Preventing Antinociceptive Tolerance and Stress-Induced Reinstatement of Extinguished Cocaine-Conditioned Place Preference

Tryptophan Substitution in CJ-15,208 (<i>cyclo</i>[Phe-D-Pro-Phe-Trp]) Introduces δ-Opioid Receptor Antagonism, Preventing Antinociceptive Tolerance and Stress-Induced Reinstatement of Extinguished Cocaine-Conditioned Place Preference

The macrocyclic tetrapeptide CJ-15,208 (<i>cyclo</i>[Phe-D-Pro-Phe-Trp]) and its D-Trp isomer exhibit kappa opioid receptor (KOR) antagonism which prevents stress-induced reinstatement of extinguished cocaine-conditioned place preference. Here, we evaluated the effects of substitution of...

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Bibliographic Details
Main Authors: Kristen H. Scherrer, Shainnel O. Eans, Jessica M. Medina, Sanjeewa N. Senadheera, Tanvir Khaliq, Thomas F. Murray, Jay P. McLaughlin, Jane V. Aldrich
Format: Article
Language:English
Published: MDPI AG 2023-08-01
Series:Pharmaceuticals
Subjects:
opioid peptides
macrocyclic tetrapeptides
multifunctional ligands
structure–activity relationships
metabolic stability
kappa opioid receptor
Online Access:https://www.mdpi.com/1424-8247/16/9/1218

Internet

https://www.mdpi.com/1424-8247/16/9/1218

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