Separation of Binding Affinity and Intrinsic Activity of the Potent μ-Opioid 14-Methoxymetopon

@article{Mahurter2006SeparationOB,
  title={Separation of Binding Affinity and Intrinsic Activity of the Potent $\mu$-Opioid 14-Methoxymetopon},
  author={Loriann Mahurter and Carrie Garceau and Jacqueline Marino and Helmut Schmidhammer and Géza Tóth and Gavril W. Pasternak},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2006},
  volume={319},
  pages={247 - 253}
}
Receptor binding studies of 5,14-O-dimethyloxymorphone (14-methoxymetopon) in brain membranes have established its high affinity for μ-binding sites, but its analgesic potency far exceeds the modest increase in binding affinity relative to other opioids. The current study has established the selectivity of [3H]14-methoxymetopon for μ sites in calf striatal membranes and for a number of full-length splice variants of the cloned murine μ-opioid receptor 1 (mMOR-1) in transfected cell lines. The… 

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