39 results found
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor

    Kathryn E Livingston et al.
    Opioid drug efficacy and allosteric modulation is measured using an active state sensor of the mu-opioid receptor.
    1. Neuroscience

    Synapse-specific opioid modulation of thalamo-cortico-striatal circuits

    William T Birdsong et al.
    By differentially modulating the two major excitatory inputs to the striatum, mu- and delta-opioid receptors regulate the balance between thalamic and cortical inputs to the striatum.
    1. Biochemistry and Chemical Biology

    Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site

    Rajendra Uprety et al.
    The structure-based design established a new approach to control pathway-selective activation of opioid receptors, resulting in new dual MOR/KOR G-protein biased agonist analgesics with attenuated liabilities.
    1. Neuroscience

    Different neuronal populations mediate inflammatory pain analgesia by exogenous and endogenous opioids

    Xin-Yan Zhang et al.
    Exogenous opioid analgesia is mediated by MORs expressed in glutamatergic neurons, whereas endogenous opioid analgesia is mediated by MORs expressed in GABAergic neurons.
    1. Neuroscience

    Visualizing endogenous opioid receptors in living neurons using ligand-directed chemistry

    Seksiri Arttamangkul et al.
    Opioid sensitive neurons were identified using a traceless affinity labeling strategy to covalently label endogenous mu-opioid receptors with fluorescent compounds in living brain slices from wild type animals.
    1. Genetics and Genomics
    2. Neuroscience

    Taar1 gene variants have a causal role in methamphetamine intake and response and interact with Oprm1

    Alexandra M Stafford et al.
    The trace amine-associated receptor 1 gene has a causal role in methamphetamine intake and thermal response, and interacts with the mu-opioid receptor gene in its methamphetamine addiction-related effects.
    1. Neuroscience

    Anti-nociceptive action of peripheral mu-opioid receptors by G-beta-gamma protein-mediated inhibition of TRPM3 channels

    Sandeep Dembla et al.
    Pro-nociceptive and pro-inflammatory TRPM3 (transient receptor potential melastatin 3) channels, expressed in somatosensory neurons, are inhibited by activation of Gαi-coupled receptors, such as µ-opioid receptors, in vitro and in vivo.
    1. Neuroscience

    Endogenous opioids in the nucleus accumbens promote approach to high-fat food in the absence of caloric need

    Kevin Caref, Saleem M Nicola
    Activation of mu-opioid receptors in the nucleus accumbens by their endogenous ligands promotes consumption of high-fat food in sated but not hungry rats, via enhancement of a neural signal that promotes cued approach behavior.
    1. Neuroscience

    Dopaminergic and opioidergic regulation during anticipation and consumption of social and nonsocial rewards

    Sebastian Korb et al.
    Administration of dopamine and opioid receptor antagonists resulted in reduced reward anticipation (effort and increased negative facial reactions), but only administration of opioid antagonists resulted in reduced liking (facial reactions).
    1. Biochemistry and Chemical Biology

    Structural and functional characterization of G protein–coupled receptors with deep mutational scanning

    Eric M Jones et al.
    Linking deep mutational scanning with engineered transcriptional reporters in human cell lines establishes a generalizable method for exploring pharmacogenomics, structure, and function across broad classes of drug receptors.

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