LP1 and LP2: Dual-Target MOPr/DOPr Ligands as Drug Candidates for Persistent Pain Relief
Molecules, 2021 Although persistent pain is estimated to affect about 20% of the adult population, current treatments have poor results. Polypharmacology, which is the administration of more than one drug targeting on two or more different sites of action, represents a ...
Lorella Pasquinucci +5 more
doaj +1 more source
Tissue distribution of messenger RNAs coding for opioid peptide precursors and related RNA. [PDF]
European Journal of Biochemistry, 1984 H. Jingami +3 more
semanticscholar +2 more sources
Ligand-Specific Regulation of the Endogenous Mu-Opioid Receptor by Chronic Treatment with Mu-Opioid Peptide Agonist [PDF]
, 2013 Since the discovery of the endomorphins (EM), the postulated endogenous peptide agonists of the mu-opioid receptors, several analogues have been synthesized to improve their binding and pharmacological profiles.
Birkás, Erika +12 more
core +3 more sources
Discovery of Kynurenines Containing Oligopeptides as Potent Opioid Receptor Agonists
Biomolecules, 2020 Kynurenine (kyn) and kynurenic acid (kyna) are well-defined metabolites of tryptophan catabolism collectively known as “kynurenines”, which exert regulatory functions in host-microbiome signaling, immune cell response, and neuronal ...
Edina Szűcs +9 more
doaj +1 more source
On the G-protein-coupled receptor heteromers and their allosteric receptor-receptor interactions in the central nervous system: focus on their role in pain modulation [PDF]
, 2013 The modulatory role of allosteric receptor-receptor interactions in the pain pathways of the Central Nervous System and the peripheral nociceptors has become of increasing interest.
Agnati, Luigi F +6 more
core +3 more sources
Drug Development and Industrial Pharmacy, 2017 Aim: In this study, self-emulsifying drug delivery system (SEDDS) for oral delivery of opioid peptide dalargin were developed and characterized in vitro.
O. Zupančič +4 more
semanticscholar +1 more source
BU10038 as a safe opioid analgesic with fewer side-effects after systemic and intrathecal administration in primates [PDF]
, 2019 © 2019 British Journal of Anaesthesia. Published by Elsevier Ltd. All rights reserved.Background: The marked increase in mis-use of prescription opioids has greatly affected our society. One potential solution is to develop improved analgesics which have
Cami-Kobeci, Gerta +9 more
core +5 more sources
High-affinity naloxone binding to filamin a prevents mu opioid receptor-Gs coupling underlying opioid tolerance and dependence. [PDF]
PLoS ONE, 2008 Ultra-low-dose opioid antagonists enhance opioid analgesia and reduce analgesic tolerance and dependence by preventing a G protein coupling switch (Gi/o to Gs) by the mu opioid receptor (MOR), although the binding site of such ultra-low-dose opioid ...
Hoau-Yan Wang +2 more
doaj +1 more source
Elucidating the active δ-opioid receptor crystal structure with peptide and small-molecule agonists
Science Advances, 2019 Crystal structures provide first atomic-level insights into δ-opioid receptor activation by two structurally diverse agonists. Selective activation of the δ-opioid receptor (DOP) has great potential for the treatment of chronic pain, benefitting from ...
T. Claff +18 more
semanticscholar +1 more source
Challenges and new opportunities for detecting endogenous opioid peptides in reward
Addiction Neuroscience, 2022 The endogenous opioid peptide system, comprised of enkephalins, endorphins, dynorphins, and nociceptin, is a highly complex neurobiological system. Opioid peptides are derived from four precursor molecules and undergo several processing events yielding ...
Sineadh M. Conway +2 more
doaj +1 more source