In vitro and in vivo Pharmacological Activities of 14-O-Phenylpropyloxymorphone, a Potent Mixed Mu/Delta/Kappa-Opioid Receptor Agonist With Reduced Constipation in Mice [PDF]
Frontiers in Pharmacology, 2018 Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Roberta Lattanzi +4 more
doaj +4 more sources
Synthesis, Biological Evaluation, and SAR Studies of 14β-phenylacetyl Substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones Derivatives: Ligands With Mixed NOP and Opioid Receptor Profile [PDF]
Frontiers in Psychiatry, 2018 A series of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydronoroxymorphinone compounds has been synthesized and evaluated for affinity and efficacy for mu (MOP), kappa (KOP), and delta (DOP) opioid receptors and nociceptin/orphanin FQ peptide (NOP ...
Vinod Kumar +6 more
doaj +6 more sources
Historical Review: Opiate Addiction and Opioid Receptors
Cell Transplantation, 2019 Substance use disorders (SUDs), defined as a collection of symptoms including tolerance and withdrawal, are chronic illnesses characterized by relapse and remission. In the United States, billions of dollars have been lost due to SUDs.
Shaocheng Wang
doaj +2 more sources
Expression and Localization of Opioid Receptors in Male Germ Cells and the Implication for Mouse Spermatogenesis. [PDF]
PLoS ONE, 2016 The presence of endogenous opioid peptides in different testicular cell types has been extensively characterized and provides evidence for the participation of the opioid system in the regulation of testicular function.
Haizea Estomba +6 more
doaj +2 more sources
Opioid Receptor-Mediated Regulation of Neurotransmission in the Brain
Frontiers in Molecular Neuroscience, 2022 Opioids mediate their effects via opioid receptors: mu, delta, and kappa. At the neuronal level, opioid receptors are generally inhibitory, presynaptically reducing neurotransmitter release and postsynaptically hyperpolarizing neurons.
Kaitlin C. Reeves +6 more
doaj +2 more sources
Molecular mechanism of biased signaling at the kappa opioid receptor
Nature Communications, 2023 The κ-opioid receptor (KOR) has emerged as an attractive drug target for pain management without addiction, and biased signaling through particular pathways of KOR may be key to maintaining this benefit while minimizing side-effect liabilities.
Amal El Daibani +13 more
semanticscholar +5 more sources
Nanobody-enabled monitoring of kappa opioid receptor states [PDF]
Nature Communications, 2020 Recent studies revealed that G protein-coupled receptors rapidly interconvert between multiple states. Here, authors use the kappa opioid receptor (KOR) and show how two state-dependent nanobodies provide real-time reporting of ligand stabilized states ...
Tao Che +13 more
doaj +4 more sources
Novel dual kappa/mu opioid ligands based on a tetrahydroisoquinoline-valine hybrid nucleus [PDF]
Scientific ReportsOpioid addiction constitutes a significant global health challenge. Kappa opioid receptor (KOP) modulators have demonstrated efficacy in treating resistant drug abuse cases.
Ahmad Abdelwaly +6 more
doaj +2 more sources
Role of kappa‐opioid and mu‐opioid receptors in pruritus: Peripheral and central itch circuits
Experimental Dermatology, 2022 Modern genetic approaches in animal models have unveiled novel itch‐specific neural pathways, emboldening a paradigm in which drugs can be developed to selectively and potently target itch in a variety of chronic pruritic conditions.
Brian S. Kim +5 more
semanticscholar +1 more source
The Kappa Opioid Receptor: A Promising Therapeutic Target for Multiple Pathologies
Frontiers in Pharmacology, 2022 Kappa-opioid receptors (KOR) are widely expressed throughout the central nervous system, where they modulate a range of physiological processes depending on their location, including stress, mood, reward, pain, inflammation, and remyelination.
Martin Dalefield +3 more
semanticscholar +1 more source