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A µ-opioid receptor modulator that works cooperatively with naloxone
The µ-opioid receptor (µOR) is a well-established target for analgesia
1 , yet conventional opioid receptor agonists cause serious adverse effects,...
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µ-Opioid receptor antagonism facilitates the anxiolytic-like effect of oxytocin in mice
Mood and anxiety disorders are leading causes of disability worldwide and are major contributors to the global burden of diseases. Neuropeptides,...
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The Kappa Opioid Receptor
This book covers the latest knowledge in structure, signaling, and biochemical pharmacology of KOR as well as preclinical research and clinical...
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Ventral tegmental area glutamate neurons establish a mu-opioid receptor gated circuit to mesolimbic dopamine neurons and regulate opioid-seeking behavior
A two-neuron model of ventral tegmental area (VTA) opioid function classically involves VTA GABA neuron regulation of VTA dopamine neurons via a mu -op...
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Opioid antagonism in humans: a primer on optimal dose and timing for central mu-opioid receptor blockade
Non-human animal studies outline precise mechanisms of central mu-opioid regulation of pain, stress, affiliation and reward processing. In humans,...
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Ptchd1 mediates opioid tolerance via cholesterol-dependent effects on μ-opioid receptor trafficking
Repeated exposure to opioids causes tolerance, which limits their analgesic utility and contributes to overdose and abuse liability. However, the...
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Profiling the proximal proteome of the activated μ-opioid receptor
The μ-opioid receptor (μOR) represents an important target of therapeutic and abused drugs. So far, most understanding of μOR activity has focused on...
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Design and structural validation of peptide–drug conjugate ligands of the kappa-opioid receptor
Despite the increasing number of GPCR structures and recent advances in peptide design, the development of efficient technologies allowing rational...
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Opioid Use Disorder
Opioid use disorder (OUD) is a significant public health burden with the highest rates of prevalence in the United States. Adverse events from...
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In vivo photopharmacology with a caged mu opioid receptor agonist drives rapid changes in behavior
Photoactivatable drugs and peptides can drive quantitative studies into receptor signaling with high spatiotemporal precision, yet few are compatible...
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Unique pharmacodynamic properties and low abuse liability of the µ-opioid receptor ligand (S)-methadone
(R,S)-methadone ((R,S)-MTD) is a µ-opioid receptor (MOR) agonist comprised of (R)-MTD and (S)-MTD enantiomers. (S)-MTD is being developed as an...
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Ligand efficacy modulates conformational dynamics of the µ-opioid receptor
The µ-opioid receptor (µOR) is an important target for pain management
1 and molecular understanding of drug action on µOR will facilitate the...
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Molecular mechanism of biased signaling at the kappa opioid receptor
The κ-opioid receptor (KOR) has emerged as an attractive drug target for pain management without addiction, and biased signaling through particular...
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Effects of the novel selective κ-opioid receptor agonist NP-5497-KA on morphine-induced reward-related behaviors
Opioid addiction and the opioid overdose epidemic are becoming more serious, and the development of therapeutic agents is essential for the...
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Off-target activity of NBOMes and NBOMe analogs at the µ opioid receptor
New psychoactive substances (NPS) are introduced on the illicit drug market at a rapid pace. Their molecular targets are often inadequately...
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Ligand and G-protein selectivity in the κ-opioid receptor
The κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not only pain but also addiction and affective disorders
1 ....
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Opioid-induced neuroanatomical, microglial and behavioral changes are blocked by suvorexant without diminishing opioid analgesia
Heroin use disorder in humans and chronic opioid administration to mice result in an increase in the number and a decrease in the size of detected...
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Targeting Peripheral μ-opioid Receptors or μ-opioid Receptor-Expressing Neurons Does not Prevent Morphine-induced Mechanical Allodynia and Anti-allodynic Tolerance
The chronic use of morphine and other opioids is associated with opioid-induced hypersensitivity (OIH) and analgesic tolerance. Among the different...
