Agonists at mu-opioid receptors spin the wheels to keep the action going.
نویسنده
چکیده
A study in this issue of Molecular Pharmacology on agonist-induced internalization of mu-opioid receptors during long-term opiate drug exposure is discussed. The study demonstrates the critical role of re-cycling of reactivated mu receptors back to the plasma membrane for the maintenance of agonist signaling during long-term opiate exposure.
منابع مشابه
Involvement of Mu Opioid Receptor Signaling in The Protective Effect of Opioid against 6-Hydroxydopamine-Induced SH-SY5Y Human Neuroblastoma Cells Apoptosis
Introduction: The neuroprotective role of opioid morphine against 6-hydroxydopamineinduced cell death has been demonstrated. However, the exact mechanism(s) underlying such neuroprotection, especially the role of subtype receptors, has not yet been fully clarified. Methods: Here, we investigated the effects of different opioid agonists on 6-OHDA-induced neurotoxicity in human neuroblastoma...
متن کاملPresynaptic mu-opioid receptors regulate a late step of the secretory process in rat ventral tegmental area GABAergic neurons.
Gamma-aminobutyric acid (GABA)-containing interneurons of the ventral tegmental area (VTA) regulate the activity of dopaminergic neurons. These GABAergic interneurons are known to be innervated by synaptic terminals containing enkephalin, an endogenous ligand of mu-opioid receptors. Bath application of mu-opioid receptor agonists inhibits the activity of VTA GABAergic neurons but the mechanism ...
متن کاملActivity of opioid ligands in cells expressing cloned mu opioid receptors
BACKGROUND The aim of the present study was to describe the activity of a set of opioid drugs, including partial agonists, in a cell system expressing only mu opioid receptors. Receptor activation was assessed by measuring the inhibition of forskolin-stimulated cyclic adenosine mono phosphate (cAMP) production. Efficacies and potencies of these ligands were determined relative to the endogenous...
متن کاملNaloxone activation of mu-opioid receptors mutated at a histidine residue lining the opioid binding cavity.
The mu-opioid receptor is the principal site of action in the brain by which morphine, other opiate drugs of abuse, and endogenous opioid peptides effect analgesia and alter mood. A member of the seven-transmembrane domain (TM) G protein-coupled receptor (GPCR) superfamily, the mu-opioid receptor modulates ion channels and second messenger effectors in an opioid agonist-dependent fashion that i...
متن کاملAgonist activation of delta-opioid receptor but not mu-opioid receptor potentiates fetal calf serum or tyrosine kinase receptor-mediated cell proliferation in a cell-line-specific manner.
Activation by opioid receptors of cell proliferation was examined with fibroblast cell lines stably expressing either delta-opioid or mu-opioid receptors. Addition of [D-Ala2, D-Leu5]-enkephalin or [D-Pen2,D-Pen5]-enkephalin to Chinese hamster ovary (CHO) cells transfected with delta-opioid receptor cDNA resulted in an agonist concentration-dependent potentiation of fetal calf serum (FCS)-stimu...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Molecular pharmacology
دوره 67 1 شماره
صفحات -
تاریخ انتشار 2005