Ligand and G-protein selectivity in the κ-opioid receptor. [PDF]
Nature, 2023 AbstractThe κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not only pain but also addiction and affective disorders1. However, the development of KOR analgesics has been hindered by the associated hallucinogenic side effects2.
Han J +13 more
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Ginsenoside Re protects methamphetamine-induced dopaminergic neurotoxicity in mice via upregulation of dynorphin-mediated κ-opioid receptor and downregulation of substance P-mediated neurokinin 1 receptor [PDF]
Journal of Neuroinflammation, 2018 Background We previously reported that ginsenoside Re (GRe) attenuated against methamphetamine (MA)-induced neurotoxicity via anti-inflammatory and antioxidant potentials.
Duy-Khanh Dang +12 more
doaj +5 more sources
Central nicotine induces browning through hypothalamic κ opioid receptor [PDF]
Nature Communications, 2019 Nicotine reduces food intake and increases energy expenditure in brown adipose tissue. Here the authors show that nicotine also induces white adipose tissue browning via central kappa opioid receptor action.
Patricia Seoane-Collazo +21 more
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The atomistic level structure for the activated human κ-opioid receptor bound to the full Gi protein and the MP1104 agonist. [PDF]
Proc Natl Acad Sci U S A, 2020 The kappa opioid receptor (κOR) is an important target for pain therapeutics to reduce depression and other harmful side effects of existing medications. The analgesic activity is mediated by κOR signaling through the adenylyl cyclase-inhibitory family of Gi protein. Here, we report the three-dimensional (3D) structure for the active state of human κOR
Mafi A, Kim SK, Goddard WA.
europepmc +11 more sources
Opioids in cancer: The κ‑opioid receptor (Review). [PDF]
Mol Med Rep, 2022 The κ-opioid receptor (KOR) is one of the primary receptors of opioids and serves a vital role in the regulation of pain, anesthesia, addiction and other pathological and physiological processes.
Zhou Q +5 more
europepmc +2 more sources
Design of κ-Opioid Receptor Agonists for the Development of Potential Treatments of Pain with Reduced Side Effects. [PDF]
Molecules, 2023 The κ-opioid receptor (KOR) has recently emerged as an alternative therapeutic target for the development of pain medications, without deleterious side effects associated with the μ-opioid receptor (MOR).
Santino F, Gentilucci L.
europepmc +2 more sources
Molecular Interaction Between Butorphanol and κ-Opioid Receptor. [PDF]
Anesth Analg, 2020 BACKGROUND: The misuse of opioids stems, in part, from inadequate knowledge of molecular interactions between opioids and opioid receptors. It is still unclear why some opioids are far more addictive than others.
Ji J +7 more
europepmc +2 more sources
Nalfurafine Hydrochloride, a κ-Opioid Receptor Agonist, Induces Melanophagy via PKA Inhibition in B16F1 Cells [PDF]
Cells, 2022 Selective autophagy controls cellular homeostasis by degrading unnecessary or damaged cellular components. Melanosomes are specialized organelles that regulate the biogenesis, storage, and transport of melanin in melanocytes.
Ha Jung Lee +13 more
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Enantiomerically Pure Quinoline-Based κ-Opioid Receptor Agonists: Chemoenzymatic Synthesis and Pharmacological Evaluation. [PDF]
ChemMedChem, 2020 AbstractRacemic K‐opioid receptor (KOR) agonist 2‐(3,4‐dichlorophenyl)‐1‐[(4aRS,8SR,8aSR)‐8‐(pyrrolidin‐1‐yl)‐3,4,4a,5,6,7,8,8a‐octahydroquinolin‐1(2H)‐yl]ethan‐1‐one ((±)‐4) was prepared in a diastereoselective synthesis. The first key step of the synthesis was the diastereoselective hydrogenation of the silyl ether of 1,2,3,4‐tetrahydroquinoin‐8‐ol ((
Martin B +6 more
europepmc +5 more sources
The κ-opioid receptor-induced autophagy is implicated in stress-driven synaptic alterations [PDF]
Frontiers in Molecular Neuroscience, 2022 Recent evidence has shown that G protein-coupled receptors (GPCRs) are direct sensors of the autophagic machinery and opioid receptors regulate neuronal plasticity and neurotransmission with an as yet unclarified mechanism.
Christos Karoussiotis +6 more
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