Opioid Receptors in Immune and Glial Cells—Implications for Pain Control [PDF]
Frontiers in Immunology, 2020 Opioid receptors comprise μ (MOP), δ (DOP), κ (KOP), and nociceptin/orphanin FQ (NOP) receptors. Opioids are agonists of MOP, DOP, and KOP receptors, whereas nociceptin/orphanin FQ (N/OFQ) is an agonist of NOP receptors.
Halina Machelska, Melih Ö. Celik
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Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors [PDF]
BMC Neuroscience, 2002 Background The aim of the present study was to characterize the activation profiles of 15 opioid ligands in transfected human embryonic kidney cells expressing only δ opioid receptors.
Clark J +3 more
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Delta-opioid receptor endocytosis in spinal cord after dermenkephalin activation [PDF]
BMC Neuroscience, 2000 Background The delta(δ)-opioid receptors belong to the G protein-coupled receptors and in vitro studies have shown that δ-opioid receptors undergo an internalization process in response to agonist stimulation.
Gastard Myriam
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Mechanistic Characterization of the Pharmacological Profile of HS-731, a Peripherally Acting Opioid Analgesic, at the µ-, δ-, κ-Opioid and Nociceptin Receptors [PDF]
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
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Synthesis, Biological Evaluation, and SAR Studies of 14β-phenylacetyl Substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones Derivatives: Ligands With Mixed NOP and Opioid Receptor Profile [PDF]
Frontiers in Psychiatry, 2018 A series of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydronoroxymorphinone compounds has been synthesized and evaluated for affinity and efficacy for mu (MOP), kappa (KOP), and delta (DOP) opioid receptors and nociceptin/orphanin FQ peptide (NOP ...
Vinod Kumar +6 more
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Opioids and opioid receptors; understanding pharmacological mechanisms as a key to therapeutic advances and mitigation of the misuse crisis [PDF]
BJA Open, 2023 Opioids are a mainstay in acute pain management and produce their effects and side effects (e.g., tolerance, opioid-use disorder and immune suppression) by interaction with opioid receptors.
David G. Lambert
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Selective targeting of mu opioid receptors to primary cilia [PDF]
Cell ReportsSummary: Opioid receptors are therapeutically important G protein-coupled receptors (GPCRs) with diverse neuromodulatory effects. The functional consequences of opioid receptor activation are known to depend on receptor location in the plasma membrane ...
Rita R. Fagan +5 more
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Pharmaceuticals, 2022 This paper proposes the design of combination opioid–adrenergic tethered compounds to enhance efficacy and specificity, lower dosage, increase duration of activity, decrease side effects, and reduce risk of developing tolerance and/or addiction ...
Robert Root-Bernstein
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Opioid Receptor-Mediated Regulation of Neurotransmission in the Brain
Frontiers in Molecular Neuroscience, 2022 Opioids mediate their effects via opioid receptors: mu, delta, and kappa. At the neuronal level, opioid receptors are generally inhibitory, presynaptically reducing neurotransmitter release and postsynaptically hyperpolarizing neurons.
Kaitlin C. Reeves +6 more
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