title: Cyclic endomorphin analogs in targeting opioid receptors to achieve pain relief.
abstract: Endomorphins, the endogenous ligands of the µ-opioid receptor, are attractive candidates for opioid-based pain-relieving agents. These tetrapeptides, with their remarkable affinity for the µ-opioid receptor, display favorable antinociceptive activity when injected directly into the brain of experimental animals. However, the application of endomorphins as clinical analgesics has been impeded by their instability in body fluids and inability to reach the brain after systemic administration. Among numerous modifications of the endomorphin structure aimed at improving their pharmacological properties, cyclization can be viewed as an interesting option. Here, we have summarized recent advances in obtaining endomorphin-based cyclic peptide analogs.
authors.affiliation: Department of Biomolecular Chemistry, Medical University of Lodz, Lodz, Poland.
authors.forename: Anna
authors.initials: A
authors.lastname: Janecka
authors.forename: Luca
authors.initials: L
authors.lastname: Gentilucci
mesh_terms: D000701:Analgesics, Opioid / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use; D000818:Animals; D001665:Binding Sites; D001812:Blood-Brain Barrier / Q000378:metabolism; D062105:Molecular Docking Simulation; D009842:Oligopeptides / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use; D010146:Pain / Q000188:drug therapy; D011957:Receptors, Opioid / Q000819:agonists* / Q000378:metabolism
chemical_list: D000701:Analgesics, Opioid; D009842:Oligopeptides; D011957:Receptors, Opioid; C105293:endomorphin 1