Potent MOR Agonists from 2′-Hydroxy-5,9-dimethyl-<i>N</i>-phenethyl Substituted-6,7-benzomorphans and from C8-Hydroxy, Methylene and Methyl Derivatives of <i>N</i>-Phenethylnormetazocine

Potent MOR Agonists from 2′-Hydroxy-5,9-dimethyl-<i>N</i>-phenethyl Substituted-6,7-benzomorphans and from C8-Hydroxy, Methylene and Methyl Derivatives of <i>N</i>-Phenethylnormetazocine

(−)-5,9-Dimethyl-6,7-benzomorphan (normetazocine) derivatives with a <i>para</i>-OH or <i>ortho</i>-F substituent in the aromatic ring of the <i>N</i>-phenethyl moiety were synthesized and found to have subnanomolar potency at MOR, and both were fully efficacious...

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Bibliographic Details
Main Authors: Madhurima Das, George W. Ward, Agnieszka Sulima, Dan Luo, Thomas Edward Prisinzano, Gregory H. Imler, Andrew T. Kerr, Arthur E. Jacobson, Kenner C. Rice
Format: Article
Language:English
Published: MDPI AG 2023-11-01
Series:Molecules
Subjects:
opioid
<i>N</i>-phenethyl analogs of 6,7-benzomorphans
<i>N</i>-phenethylnormetazocine derivatives
C8-alkyl substituted 6,7-benzomorphans
C8-alkenyl substituted 6,7-benzomorphans
inhibition of forskolin-induced cAMP accumulation assay (cAMP assay)
Online Access:https://www.mdpi.com/1420-3049/28/23/7709

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