Mu-opioid receptor agonists represent mainstays of pain management. However, the therapeutic use of these agents is associated with serious side effects, including potentially lethal respiratory depression.
Andrew C. Kruegel+7 more
semanticscholar +1 more source
AAV gene therapy vectors in the TMJ
Abstract Objectives The goal of this project was to evaluate the use of two adeno‐associated viral vector serotypes, adeno‐associated viral vectors (AAV)‐2 and AAV‐6, approved for and used for gene therapy in humans, for the delivery of therapeutic genes to the temporomandibular joint (TMJ) and the attendant sensory nerves.
Sabine M. Brouxhon+2 more
wiley +1 more source
Biased agonists of the kappa opioid receptor may relieve intractable itch without causing unwanted side effects. Itch relief from biased agonists Activating the kappa opioid receptor (KOR) can relieve itching that is not caused by allergic reactions ...
Tarsis F. Brust+13 more
semanticscholar +1 more source
GRKs as Key Modulators of Opioid Receptor Function
Understanding the link between agonist-induced phosphorylation of the mu-opioid receptor (MOR) and the associated physiological effects is critical for the development of novel analgesic drugs and is particularly important for understanding the ...
Laura Lemel+2 more
doaj +1 more source
The Efficacy of Peripheral Opioid Antagonists in Opioid-Induced Constipation and Postoperative Ileus: A Systematic Review of the Literature. [PDF]
Opioid-induced constipation has a negative impact on quality of life for patients with chronic pain and can affect more than a third of patients. A related but separate entity is postoperative ileus, which is an abnormal pattern of gastrointestinal ...
Baratta, Jaime L.+5 more
core +1 more source
Modulation of Neurally Mediated Vasodepression and Bradycardia by Electroacupuncture through Opioids in Nucleus Tractus Solitarius. [PDF]
Stimulation of vagal afferent endings with intravenous phenylbiguanide (PBG) causes both bradycardia and vasodepression, simulating neurally mediated syncope.
Fu, Liang-Wu+3 more
core +3 more sources
Crystal structure of the μ-opioid receptor bound to a morphinan antagonist
Opium is one of the world’s oldest drugs, and its derivatives morphine and codeine are among the most used clinical drugs to relieve severe pain. These prototypical opioids produce analgesia as well as many undesirable side effects (sedation, apnoea and ...
A. Manglik+9 more
semanticscholar +1 more source
Prefrontal FGF1 Signaling is Required for Accumbal Deep Brain Stimulation Treatment of Addiction
This research delineates that a cortical‐accumbal pathway and local FGF1 signaling in the medial prefrontal cortex are critical for NAc‐DBS to be effective in altering morphine CPP. These findings demonstrate a top‐down motif to regulate the therapeutic effects of subcortical DBS on addiction and support the potential for addiction treatments involving
Wan‐Kun Gong+11 more
wiley +1 more source
High-affinity naloxone binding to filamin a prevents mu opioid receptor-Gs coupling underlying opioid tolerance and dependence. [PDF]
Ultra-low-dose opioid antagonists enhance opioid analgesia and reduce analgesic tolerance and dependence by preventing a G protein coupling switch (Gi/o to Gs) by the mu opioid receptor (MOR), although the binding site of such ultra-low-dose opioid ...
Hoau-Yan Wang+2 more
doaj +1 more source
Opioid regulation of Mu receptor internalisation: relevance to the development of tolerance and dependence [PDF]
Internalisation of the mu opioid receptor from the surface of cells is generally achieved by receptor occupancy with agonist ligands of high efficacy. However, in many situations the potent analgesic morphine fails to promote internalisation effectively ...
Lopez-Gimenez, J.F., Milligan, G.
core +2 more sources