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A Photochromic Agonist for μ‐Opioid Receptors
Angewandte Chemie International Edition, 2014AbstractOpioid receptors (ORs) are widely distributed in the brain, the spinal cord, and the digestive tract and play an important role in nociception. All known ORs are G‐protein‐coupled receptors (GPCRs) of family A. Another well‐known member of this family, rhodopsin, is activated by light through the cis/trans isomerization of a covalently bound ...
Matthias Schönberger, Dirk Trauner
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Opioid Agonists and Antagonists
2021Pain causes severe limitation of human functionality and productivity. Humans have waged a long war against pain using different forms of analgesics. Among the different forms of analgesics, opiates are a class of drugs which has been the most promising in the treatment of pain. The natural opiates are derived from the resin of the poppy plant (Papaver
Shathish Kumar, Soumya Itagi
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Highlights in opioid agonists and antagonists
Expert Review of Neurotherapeutics, 2006This review highlights new insights in to opioid agonists and antagonists, focusing on their mechanism of action with spinal and systemic administration, chronic use and main adverse effects. Short-cuts on some opioid agonists and antagonists of clinical interest are also presented, revealing potential clinical implications and future clinical ...
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The duration dilemma in opioid agonist therapy
Journal of Opioid Management, 2021Objective: Studies dating back to 1964 consistently support the effectiveness of methadone as a maintenance treatment for opioid use disorder (OUD), and since 2003, the effectiveness of buprenorphine. Short-term detoxification has not proven to be an effective treatment, as it results in high relapse rates when compared with maintenance treatment with ...
Anjali, Dhanda, Edwin A, Salsitz
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Emerging Field of Biased Opioid Agonists
Anesthesiology Clinics, 2023Advances in opioid pharmacology promise to bring a "better opioid." Biased opioid agonists, designed to recruit G protein over β-arrestin signaling, may provide analgesia without adverse effects of traditional opioids. Oliceridine, the first biased opioid agonist, was approved in 2020.
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Opioid agonist treatment for people who are dependent on pharmaceutical opioids
Cochrane Database of Systematic Reviews, 2022There are ongoing concerns regarding pharmaceutical opioid-related harms, including overdose and dependence, with an associated increase in treatment demand. People dependent on pharmaceutical opioids appear to differ in important ways from people who use heroin, yet most opioid agonist treatment research has been conducted in people who use heroin ...
Suzanne, Nielsen +2 more
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Interleukins Counteract Opioid Agonists Immunosuppression
International Journal of Neuroscience, 1990A centrally acting novel analgesic, PM, added to murine lymphocyte cultures abrogated the mitogenic response to Con A, as well as, interleukin 2 production, in a dose-dependent manner. Simultaneous presence of interleukin 1 (IL-1) and interleukin 2 (IL-2) into the cultures counteracted, in a dose-dependent manner, as naloxone does, the ...
E E, Karagouni +1 more
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Immunosuppression by a Novel Analgesic‐Opioid Agonist
Scandinavian Journal of Immunology, 1989The effect of a new, centrally acting analgesic, 2‐n‐pentyloxy‐2‐phenyl‐4‐methyl‐morpholine (PM) on the humoral antibody isotype responses, mitogenic responses, and interleukin production and assay was studied. Treatment with this opioid agonist exerted a suppressive effect on the antibody responses to TD [sheep red blood cells (SRBC), fluoresceinated ...
L, Hadjipetrou-Kourounakis +3 more
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New opioid receptor modulators and agonists
Best Practice & Research Clinical Anaesthesiology, 2018There has been significant research to develop an ideal synthetic opioid. Opioids with variable properties possessing efficacy and with reduced side effects have been synthesized when compared to previously used agents. An opioid modulator is a drug that can produce both agonistic and antagonistic effects by binding to different opioid receptors and ...
Alan D, Kaye +8 more
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