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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: | 2019-02-15T16:54:10Z |
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