Molecules, 2022 Accumulated preclinical and clinical data show that peripheral restricted opioids provide pain relief with reduced side effects. The peripherally acting opioid analgesic HS-731 is a potent dual μ-/δ-opioid receptor (MOR/DOR) full agonist, and a weak ...
Kristina Puls +3 more
doaj +1 more source
Nature Communications, 2019 Opioid analgesics are powerful pain relievers; however, over time, pain control diminishes as analgesic tolerance develops. The molecular mechanisms initiating tolerance have remained unresolved to date.
A. Kliewer +8 more
semanticscholar +1 more source
Binding mode analyses of NAP derivatives as mu opioid receptor selective ligands through docking studies and molecular dynamics simulation [PDF]
, 2017 Mu opioid receptor selective antagonists are highly desirable because of their utility as pharmacological probes for receptor characterization and functional studies.
Wang, Huiqun +2 more
core +2 more sources
The Role of Opioid Receptors in Immune System Function
Frontiers in Immunology, 2019 Research on the effects of opioids on immune responses was stimulated in the 1980s by the intersection of use of intravenous heroin and HIV infection, to determine if opioids were enhancing HIV progression.
T. Eisenstein
semanticscholar +1 more source
In vitro and in vivo pharmacological activities of 14-o-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice [PDF]
, 2018 Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Lattanzi, Roberta +4 more
core +2 more sources
Morphine activates neuroinflammation in a manner parallel to endotoxin [PDF]
, 2012 Opioids create a neuroinflammatory response within the CNS, compromising opioid-induced analgesia and contributing to various unwanted actions. How this occurs is unknown but has been assumed to be via classic opioid receptors.
A. A. Somogyi +42 more
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Opioid regulation of Mu receptor internalisation: relevance to the development of tolerance and dependence [PDF]
, 2010 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
BU10038 as a safe opioid analgesic with fewer side-effects after systemic and intrathecal administration in primates [PDF]
, 2019 © 2019 British Journal of Anaesthesia. Published by Elsevier Ltd. All rights reserved.Background: The marked increase in mis-use of prescription opioids has greatly affected our society. One potential solution is to develop improved analgesics which have
Cami-Kobeci, Gerta +9 more
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Dopamine-D1 and δ-opioid receptors co-exist in rat striatal neurons [PDF]
, 2006 Cocaine’s enhancement of dopaminergic neurotransmission in the mesolimbic pathway plays a critical role in the initial reinforcing properties of this drug. However, other neurotransmitter systems are also integral to the addiction process.
Ambrose-Lanci, L. M. +3 more
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