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EnglishHerein 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 molecular docking analysis. Hence, H-Tyr-Amo-Trp-PheNH2 resulted to be a new chemotype of highly stable, selective, partial KOR agonist inducing analgesia, therefore displaying great potential interest as a painkiller possibly with reduced harmful side effects.
| Titolo: | Constraining Endomorphin-1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ-Opioid Receptor Selective Partial Agonist | |
| Autore/i: | De Marco, Rossella; Bedini, Andrea; Spampinato, Santi; Comellini, Lorenzo; Zhao, Junwei; Artali, Roberto; Gentilucci, Luca | |
| Autore/i Unibo: | ||
| Anno: | 2018 | |
| Rivista: | ||
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1021/acs.jmedchem.8b00296 | |
| Abstract: | 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 molecular docking analysis. Hence, H-Tyr-Amo-Trp-PheNH2 resulted to be a new chemotype of highly stable, selective, partial KOR agonist inducing analgesia, therefore displaying great potential interest as a painkiller possibly with reduced harmful side effects. | |
| Data stato definitivo: | 2021-02-25T12:49:24Z | |
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