19 results found
    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. Medicine
    2. Neuroscience

    Respiratory depression and analgesia by opioid drugs in freely behaving larval zebrafish

    Shenhab Zaig et al.
    Emerging approaches in larval zebrafish to identify safe opioid therapies without the side-effect of respiratory depression.
    1. Neuroscience

    Opioids depress breathing through two small brainstem sites

    Iris Bachmutsky et al.
    Opioids stop breathing during overdose by silencing two small brain sites, with just 140 neurons in the breathing rhythm generator exerting the key effect.
    1. Neuroscience

    Polyglycerol-opioid conjugate produces analgesia devoid of side effects

    Sara González-Rodríguez et al.
    A novel opioid formulation producing analgesia similar to conventional opioids without permeation of blood-brain or intestinal barriers, thus precluding sedation, constipation and respiratory depression.
    1. Neuroscience

    Medical education and distrust modulate the response of insular-cingulate network and ventral striatum in pain diagnosis

    Giada Dirupo et al.
    Behavioral and neural data converge in showing that medical experience reduces reactions to others' pain and distrust toward the target affects the processing of his feedback.
    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.
    1. Neuroscience

    Antinociceptive modulation by the adhesion GPCR CIRL promotes mechanosensory signal discrimination

    Sven Dannhäuser et al.
    An interdisciplinary approach uncovers a new antinociceptive molecular mechanism and shows that the adhesion GPCR CIRL adjusts the sensation of gentle touch and noxious mechanical insult in opposite directions.
    1. Cell Biology
    2. Medicine

    Senotherapeutic drugs for human intervertebral disc degeneration and low back pain

    Hosni Cherif et al.
    Targeting senescent cells in human intervertebral discs, using senotherapeutics, provides a potential therapeutic strategy to prevent or reduce disc degeneration and pain.
    1. Neuroscience

    Upregulation of TRPM3 in nociceptors innervating inflamed tissue

    Marie Mulier et al.
    The expression and function of the cation channel TRPM3 is strongly increased in sensory neurons innervating inflamed tissue, likely contributing to inflammatory hyperalgesia and persistent pain.
    1. Neuroscience

    MRGPRX4 is a bile acid receptor for human cholestatic itch

    Huasheng Yu et al.
    Bile acid and it's receptor MRGPRX4, but not TGR5, is one of the ligand-receptor pairs for chronic itch in patients with liver diseases.

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