Design, Synthesis, and Characterization of Novel, Subtype-Selective Fluorescent Antagonists Targeting the Nociceptin/Orphanin FQ Opioid Peptide Receptor.

ABSTRACT: The nociceptin/orphanin FQ opioid peptide receptor (NOPr) is a member of the opioid receptor family under investigation for the treatment of depression, Parkinson's disease, addiction, and pain. Opioid analgesics such as morphine act through μ-opioid receptor (MOPr) activation but cause MOPr-driven side effects that include respiratory depression, tolerance, addiction, and constipation. Bivalent NOPr/MOPr agonists have been shown to confer effective analgesia with an improved side effect profile. However, the development of new NOPr-targeting drugs is challenged by a paucity of pharmacological tools to characterize NOPr-ligands and visualize receptor expression. We report the design, synthesis, and pharmacological evaluation of the first high affinity small molecule NOPr-targeting fluoresc

SUBMITTER: Farmer GJ 

PROVIDER: S-EPMC12833874 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature