Constraining Endomorphin‑1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ‑Opioid Receptor Selective Partial Agonist

Herein we present the expedient synthesis of endomorphin-1 analogues containing stereoisomeric β2-homo-Freidinger lactam-like scaffolds ([Amo2]EM), and we discuss opioid receptor (OR) affinity, enzymatic stability, functional activity, in vivo antinociceptive effects, and conformational and molecul...

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Veröffentlicht in:	Journal of medicinal chemistry 2018-07, Vol.61 (13), p.5751-5757
Hauptverfasser:	De Marco, Rossella, Bedini, Andrea, Spampinato, Santi, Comellini, Lorenzo, Zhao, Junwei, Artali, Roberto, Gentilucci, Luca
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics - chemical synthesis Analgesics - chemistry Analgesics - metabolism Analgesics - pharmacology Animals Dipeptides - chemistry Heterocyclic Compounds - chemistry Mice Molecular Docking Simulation Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - metabolism Oligopeptides - pharmacology Protein Conformation Receptors, Opioid, kappa - agonists Receptors, Opioid, kappa - chemistry Receptors, Opioid, kappa - metabolism
Online-Zugang:	Volltext
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