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Involvement of Mitogen-Activated Protein Kinase in Agonist-Induced Phosphorylation of the μ-Opioid Receptor in HEK 293 Cells by Harald Schmidt; Stefan Schulz; Marcus Klutzny; Thomas Koch; Manuela Händel; Volker Höllt is a Neuroscience article available to read on EtoBox.

What is Involvement of Mitogen-Activated Protein Kinase in Agonist-Induced Phosphorylation of the μ-Opioid Receptor in HEK 293 Cells about?

**Abstract:** Agonist exposure of many G protein‐coupled receptors stimulates an activation of extracellular signal‐regulated protein kinases (ERKs) 1 and 2, members of the mitogen‐activated protein kinase (MAPK) family. Here, we show that treatment of human embryonic kidney (HEK) 293 cells stably transfected to express the rat μ‐opioid receptor (MOR1) with [D‐Ala^2^,MePhe^4^,Gly^5^‐ol]enkephalin (DAMGO) stimulated a rapid and transient (3‐5‐min) activation and nuclear translocation of MAPK. Exposure of these cells to the MAPK kinase 1 inhibitor PD98059 not only prevented MAPK activation but also inhibited homologous desensitization of the μ‐opioid receptor. We have therefore determined the effect of PD98059 on agonist‐induced μ‐receptor phosphorylation. DAMGO stimulated a threefold increase in MOR1 phosphorylation within 20 min that could be reversed by the antagonist naloxone. PD98059 produced a dose‐dependent inhibition of agonist‐promoted μ‐receptor phosphorylation with an IC~50~ of 20 μ__M__. DAMGO also induced MOR1 internalization that peaked at 30 min. Confocal microscopy revealed that DAMGO‐induced MOR1 internalization was also largely inhibited in the presence of PD98059.

Who reads Involvement of Mitogen-Activated Protein Kinase in Agonist-Induced Phosphorylation of the μ-Opioid Receptor in HEK 293 Cells?

Author

Harald Schmidt; Stefan Schulz; Marcus Klutzny; Thomas Koch; Manuela Händel; Volker Höllt

Publisher

John Wiley and Sons; Wiley (Blackwell Publishing); Blackwell Publishing Inc.; Wiley (ISSN 0022-3042)

Published

2000

Language

EN

Field

Neuroscience (Life Sciences)