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Molecular mechanisms and regulation of opioid receptor signaling.
In the current review, recent advances in the delineation basis for the multiple opioid receptor signaling, and their regulation at multiple levels are examined. Expand
Unidirectional Cross-Activation of GRPR by MOR1D Uncouples Itch and Analgesia Induced by Opioids
It is suggested that opioid-induced itch is an active process concomitant with but independent of opioid analgesia, occurring via the unidirectional cross-activation of GRPR signaling by MOR1D heterodimerization. Expand
Phosphorylation of Ser363, Thr370, and Ser375 Residues within the Carboxyl Tail Differentially Regulates μ-Opioid Receptor Internalization*
The present data show that the basal phosphorylation of MOR could play a role in modulating agonist-induced receptor internalization kinetics, and even though μ-receptors and δ-opioid receptors have the same motif encompassing agonists-induced phosphorylated sites, the different agonists' internalization properties controlled by these sites suggest differential cellular regulation of these two receptor subtypes. Expand
β-Arrestin-Dependent μ-Opioid Receptor-Activated Extracellular Signal-Regulated Kinases (ERKs) Translocate to Nucleus in Contrast to G Protein-Dependent ERK Activation
The cellular location of phosphorylated ERKs and subsequent activities on gene transcriptions are dictated by the agonist used to activate the receptor and the subsequent signaling pathway involved. Expand
delta-Opioid receptor immunoreactivity: distribution in brainstem and spinal cord, and relationship to biogenic amines and enkephalin
A delta- opioid receptor may affect the activity of descending serotoninergic and noradrenergic neurons by means of modulating the release of neurotransmitters from afferents to these neurons. Expand
Immunofluorescent identification of a delta (delta)-opioid receptor on primary afferent nerve terminals.
Interestingly, terminals containing DOR-1-ir appeared to be closely apposed by fibers and terminals containing enkephalin (ENK)-ir, which suggests that ENK may be a physiologically relevant ligand for the receptor encoded by D OR-1, and that DORN may act to regulate the release of transmitters from small diameter primary afferent neurons. Expand
The kappa-opioid receptor is primarily postsynaptic: combined immunohistochemical localization of the receptor and endogenous opioids.
The results suggest that the KOR1 protein is primarily, but not exclusively, deployed to postsynaptic membranes where it mediates the effects of products of preprodynorphin and possibly preproenkephalin. Expand
U73122 inhibits phospholipase C-dependent calcium mobilization in neuronal cells
The results are consistent with U73122 inhibiting PLC in neuronal cells and indicate that under the appropriate conditions, this compound is a useful tool for studying inositol 1,4,5-trisphosphate (IP3)-mediated Ca2+ mobilization. Expand
Spinal G-Protein-Gated Potassium Channels Contribute in a Dose-Dependent Manner to the Analgesic Effect of μ- and δ- But Not κ-Opioids
Opioids can evoke analgesia by inhibiting neuronal targets in either the brain or spinal cord, and multiple presynaptic and postsynaptic inhibitory mechanisms have been implicated. The relativeExpand
Receptor density and recycling affect the rate of agonist-induced desensitization of mu-opioid receptor.
The ability of the mu-opioid receptor to resensitize and to recycle, and the relative efficiency of the receptor to regulate adenylyl cyclase activity, contributed to the observed slow rate of mu-operative receptor desensitization in HEK293 cells. Expand