The Intriguing Effects of Substituents in the <i>N</i>-Phenethyl Moiety of Norhydromorphone: A Bifunctional Opioid from a Set of “Tail Wags Dog” Experiments

The Intriguing Effects of Substituents in the <i>N</i>-Phenethyl Moiety of Norhydromorphone: A Bifunctional Opioid from a Set of “Tail Wags Dog” Experiments

(−)-<i>N</i>-Phenethyl analogs of optically pure <i>N</i>-norhydromorphone were synthesized and pharmacologically evaluated in several in vitro assays (opioid receptor binding, stimulation of [<sup>35</sup>S]GTPγS binding, forskolin-induced cAMP accumulation assay...

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Main Authors: Meining Wang, Thomas C. Irvin, Christine A. Herdman, Ramsey D. Hanna, Sergio A. Hassan, Yong-Sok Lee, Sophia Kaska, Rachel Saylor Crowley, Thomas E. Prisinzano, Sarah L. Withey, Carol A. Paronis, Jack Bergman, Saadet Inan, Ellen B. Geller, Martin W. Adler, Theresa A. Kopajtic, Jonathan L. Katz, Aaron M. Chadderdon, John R. Traynor, Arthur E. Jacobson, Kenner C. Rice
Format: Article
Language:English
Published: MDPI AG 2020-06-01
Series:Molecules
Subjects:
opioid
bifunctional ligands
(−)-<i>N</i>-phenethylnorhydromorphone analogs
[<sup>35</sup>S]GTPgammaS assay
forskolin-induced cAMP accumulation assays
β-arrestin recruitment assays
Online Access:https://www.mdpi.com/1420-3049/25/11/2640

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