Agonist-induced functional desensitization of the mu-opioid receptor is mediated by loss of membrane receptors rather than uncoupling from G protein.

@article{Pak1996AgonistinducedFD,
  title={Agonist-induced functional desensitization of the mu-opioid receptor is mediated by loss of membrane receptors rather than uncoupling from G protein.},
  author={Youngshil Pak and A Kouvelas and Mark A Scheideler and Julia Rasmussen and Brian F O'dowd and Susan R. George},
  journal={Molecular pharmacology},
  year={1996},
  volume={50 5},
  pages={
          1214-22
        }
}
The effects of acute exposure of the opioid peptide [D-Ala2,N-MePhe4, Gly-ol5]enkephalin (DAMGO) on the mu-opioid receptor were examined in Chinese hamster ovary (CHO) K-1 and baby hamster kidney stable transfectants. In the CHO cell line, acute 1-hr treatment with DAMGO decreased the density of receptors without affecting the affinity or proportion of agonist-detected sites and attenuated the ability of the agonist to inhibit forskolin-stimulated cAMP accumulation. In contrast, similar 1-hr… CONTINUE READING

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The opioidergic system: potential roles and therapeutic indications in the eye.

Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics • 2008