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Opioid Affinity of Diazacyclic Peptidomimetic Compounds Derived from Reduced Polyamides
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Opioid Affinity of Diazacyclic Peptidomimetic Compounds Derived from Reduced Polyamides
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Journal Article
Opioid Affinity of Diazacyclic Peptidomimetic Compounds Derived from Reduced Polyamides
2025
Overview
Diaza-peptidomimetics are constrained compounds that mimic the biological efficacy of peptides while offering increased stability. We have previously reported the synthesis of bis-cyclic guanidine heterocyclic peptidomimetics as opioid ligands with mixed μ-, κ- and δ-opioid receptor interactions and their potential activity as novel analgesics. Using the same approach, we report here the synthesis of sulfonated and piperazine-tethered bis-cyclic guanidines and their in vitro screening results from radioligand competition binding assays at the μ- (MOR), δ- (DOR), and κ- (KOR) opioid receptors.
Publisher
MDPI AG
Subject
/ Analgesics, Opioid - chemistry
/ Analgesics, Opioid - metabolism
/ Analgesics, Opioid - pharmacology
/ Animals
/ Cocaine
/ Humans
/ Ligands
/ Morphine
/ Nonsteroidal anti-inflammatory drugs
/ Pain
/ Peptidomimetics - chemical synthesis
/ Peptidomimetics - metabolism
/ Peptidomimetics - pharmacology
/ Receptors, Opioid - metabolism
/ Receptors, Opioid, delta - metabolism
