Morphine induces terminal micro-opioid receptor desensitization by sustained phosphorylation of serine-375

• Published in: The EMBO journal Vol. 23; no. 16; pp. 3282 - 3289
• Main Authors: Schulz, Stefan, Mayer, Dana, Pfeiffer, Manuela, Stumm, Ralf, Koch, Thomas, Höllt, Volker
• Format: Journal Article
• Language: English
• Published: England 18.08.2004
• Subjects: Cell Line; Enkephalin, Ala-MePhe-Gly- - pharmacology; Humans; Morphine - pharmacology; Mutation - genetics; Phosphorylation - drug effects; Phosphoserine - metabolism; Receptors, Opioid, mu - genetics; Receptors, Opioid, mu - metabolism

Morphine is a poor inducer of micro-opioid receptor (MOR) internalization, but a potent inducer of cellular tolerance. Here we show that, in contrast to full agonists such as [D-Ala(2)-MePhe(4)-Gly-ol]enkephalin (DAMGO), morphine stimulated a selective phosphorylation of the carboxy-terminal residue...