Discovery of Potent Kappa Opioid Receptor Agonists Derived from Akuammicine [PDF]
J Med ChemAkuammicine (1), an indole alkaloid isolated from the seeds of Picralima nitida, is a selective agonist of the kappa opioid receptor (κOR). To establish structure-activity relationships (SAR) for this structurally unique κOR ligand, a collection of 26 ...
Anna M., Gutridge +5 more
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Structural dynamics of kappa opioid receptor interactions with β-arrestin 1 [PDF]
Nature CommunicationsOpioid receptors signal through Gi/o protein and β-arrestin pathways that mediate distinct effects of opiate drugs. While opioid binding and G protein activation are well studied, β-arrestin recruitment remains poorly understood.
Jianming Han +15 more
doaj +2 more sources
Molecular mechanism of biased signaling at the kappa opioid receptor [PDF]
Nature Communications, 2023 Biased signaling in κ-opiod receptors (KOR) offer an attractive strategy for pain management. Here the authors identify determinants of KOR signaling bias using structural methods in combination with molecular dynamics simulations.
Amal El Daibani +13 more
doaj +2 more sources
Signaling underlying kappa opioid receptor-mediated behaviors in rodents [PDF]
Frontiers in Neuroscience, 2022 Kappa opioid receptor (KOR) agonists are potentially useful as analgesic and anti-pruritic agents, for prevention and treatment of substance use disorders, and for treatment of demyelinating diseases.
Lee-Yuan Liu-Chen, Peng Huang
doaj +2 more sources
Renal Implications of Kappa Opioid Receptor Signaling in Sprague-Dawley Rats [PDF]
FunctionOpioid use for pain management and illicit consumption has been associated with adverse cardiovascular and cardiorenal outcomes. Despite these associations, the mechanisms underlying opioid-induced kidney damage remain poorly understood.
Steven Didik +11 more
doaj +2 more sources
Mapping Kappa Opioid Receptor Binding in Titi Monkeys with [C]GR103545 PET [PDF]
Molecular ImagingPurpose The kappa opioid receptor (KOR) plays a pivotal role in stress- and anxiety-related behaviors, with growing evidence linking it to stress induced by social isolation and separation.
Alita Jesal D Almeida BEng +6 more
doaj +2 more sources
Exploring the role of mu opioid receptor (OPRM1) and CYP2B6 gene variations for methadone pharmacogenomics. Can these variations be used to advance toxicological interpretation post-mortem?. [PDF]
Methadone is increasingly involved in drug overdose cases and the molecular actions of the drug in vivo are largely unknown requiring elucidation. This study set out to examine the relationship between methadone toxicity and CYP2B6 and mu (μ) opioid ...
Bunten, Hannah
core +9 more sources
6,5-Fused Ring, C2-Salvinorin Ester, Dual Kappa and Mu Opioid Receptor Agonists as Analgesics Devoid of Anxiogenic Effects [PDF]
, 2021 Analgesia is commonly mediated through the mu or kappa opioid receptor agonism. Unfortunately, selective mu or kappa receptor agonists often cause harmful side effects.
Adam W., Keasling +9 more
core +2 more sources
Asymmetric syntheses of (+)- and (–)-collybolide enable reevaluation of kappa-opioid receptor agonism [PDF]
, 2022 The fungal metabolite collybolide attracted attention as a non-nitrogenous, potent and biased agonist of the kappa-opioid receptor (KOR). Here we report a 10-step asymmetric synthesis of this complex sesquiterpene that enables facile access to either ...
Stephan, Freeman +5 more
core +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.
Murányi Marianna +25 more
core +2 more sources