Pharmacological Profiles of Oligomerized μ-Opioid Receptors
Opioids are widely prescribed pain relievers with multiple side effects and potential complications. They produce analgesia via G-protein-protein coupled receptors: μ-, δ-, κ-opioid and opioid receptor-like 1 receptors.
Ing-Kang Ho, Cynthia Wei-Sheng Lee
doaj +3 more sources
The Peptide PnPP-19, a Spider Toxin Derivative, Activates μ-Opioid Receptors and Modulates Calcium Channels [PDF]
The synthetic peptide PnPP-19 comprehends 19 amino acid residues and it represents part of the primary structure of the toxin δ-CNTX-Pn1c (PnTx2-6), isolated from the venom of the spider Phoneutria nigriventer.
Ana C. N. Freitas +11 more
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Opioid receptor distribution in the claustrum-dorsal endopiriform complex [PDF]
Summary: The claustrum and dorsal endopiriform form a subcortical structure reciprocally connected to the neocortex and enriched in opioid receptors. However, the precise cellular distribution of opioid receptors within this region remains unclear. Using
Matthew Bolger +2 more
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Beta1 subunits enable fentanyl-induced BK channel activation and opioid regulation of cerebral artery diameter. [PDF]
During the current opioid crisis, the majority of overdose deaths are attributed to ultra‐potent synthetic opioids, such as fentanyl. While fentanyl exerts its action via opioid receptors, we propose that potassium channels in the brain blood vessels may also sense fentanyl.
Thapa S +4 more
europepmc +2 more sources
EphB1 Receptor Blockade Augments Morphine Antinociception via Inhibiting GRK2-Mediated µ-Opioid Receptor Internalization. [PDF]
Administration of opioids activates ephrinB2‐EphB1 receptor signaling. Activated EphB1 receptors induce GRK2‐mediated phosphorylation of MOR at Ser375, which initiates the internalization of MOR and reduces opioid antinociception at the behavioral level. ABSTRACT Opioids are the primary treatment for severe pain in clinical practice.
Peng B +7 more
europepmc +2 more sources
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
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
doaj +1 more source
Opioid receptors are members of the group of G protein-couple receptors, which have been proven to be effective targets for treating severe pain. The interactions between the opioid receptors and corresponding ligands and the receptor’s activation by ...
Peng Xie +8 more
doaj +1 more source
Bidirectional Regulation of Opioid and Chemokine Function
The opioid family of GPCRs consists of the classical opioid receptors, designated μ-, κ-, and δ-opioid receptors, and the orphanin-FQ receptor, and these proteins are expressed on both neuronal and hematopoietic cells.
Thomas J. Rogers
doaj +1 more source
Ligand-Specific Regulation of the Endogenous Mu-Opioid Receptor by Chronic Treatment with Mu-Opioid Peptide Agonist [PDF]
Since the discovery of the endomorphins (EM), the postulated endogenous peptide agonists of the mu-opioid receptors, several analogues have been synthesized to improve their binding and pharmacological profiles.
Murányi Marianna +25 more
core +2 more sources

