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Opioid bifunctional ligands from morphine and the opioid pharmacophore Dmt-Tic

By Balboni G., Salvadori S., Marczak E.D., Knapp B.I., Bidlack J.M., Lazarus L. H., Peng X. and Si G.Y. Neumeyer.


Bifunctional ligands containing an ester linkage between morphine and the d-selective pharmacophore Dmt-Tic were synthesized, and their binding affinity and functional bioactivity at the m, d and k opioid receptors determined. Bifunctional ligands containing or not a spacer of b-alanine between the two pharmacophores lose the m agonism deriving from morphine becoming partial m agonists 4 or m antagonists 5. Partial k agonism is evidenced only for compound 4. Finally, both compounds showed potent d antagonis

Topics: Bifunctional ligands\ud Dmt-Tic pharmacophore\ud Opioid receptors
Year: 2011
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