Constitutive activity of the cannabinoid CB1 receptor regulates the function of co-expressed Mu opioid receptors.

@article{Canals2008ConstitutiveAO,
  title={Constitutive activity of the cannabinoid CB1 receptor regulates the function of co-expressed Mu opioid receptors.},
  author={Meritxell Canals and Graeme Milligan},
  journal={The Journal of biological chemistry},
  year={2008},
  volume={283 17},
  pages={11424-34}
}
The human mu opioid receptor was expressed stably in Flp-In T-REx HEK293 cells. Occupancy by the agonist DAMGO (Tyr-d-Ala-Gly-N-methyl-Phe-Gly-ol) resulted in phosphorylation of the ERK1/2 MAP kinases, which was blocked by the opioid antagonist naloxone but not the cannabinoid CB1 receptor inverse agonist SR141716A. Expression of the human cannabinoid CB1 receptor in these cells from the inducible Flp-In T-REx locus did not alter expression levels of the mu opioid receptor. This allowed the… CONTINUE READING

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