Design, Synthesis, and In Vitro Characterization of Proteolytically-Stable Opioid-Neurotensin Hybrid Peptidomimetics.
Autor: | De Neve J; Research Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel, 1050 Brussels, Belgium., Breault É; Institut de Pharmacologie de Sherbrooke, Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12e Avenue Nord, J1H 5N4 Sherbrooke, Quebec, Canada., Previti S; Research Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel, 1050 Brussels, Belgium., Vangeloven E; Research Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel, 1050 Brussels, Belgium., Loranger B; Institut de Pharmacologie de Sherbrooke, Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12e Avenue Nord, J1H 5N4 Sherbrooke, Quebec, Canada., Chartier M; Institut de Pharmacologie de Sherbrooke, Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12e Avenue Nord, J1H 5N4 Sherbrooke, Quebec, Canada., Brouillette R; Institut de Pharmacologie de Sherbrooke, Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12e Avenue Nord, J1H 5N4 Sherbrooke, Quebec, Canada., Lanoie A; Institut de Pharmacologie de Sherbrooke, Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12e Avenue Nord, J1H 5N4 Sherbrooke, Quebec, Canada., Holleran BJ; Institut de Pharmacologie de Sherbrooke, Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12e Avenue Nord, J1H 5N4 Sherbrooke, Quebec, Canada., Longpré JM; Institut de Pharmacologie de Sherbrooke, Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12e Avenue Nord, J1H 5N4 Sherbrooke, Quebec, Canada., Gendron L; Institut de Pharmacologie de Sherbrooke, Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12e Avenue Nord, J1H 5N4 Sherbrooke, Quebec, Canada., Tourwé D; Research Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel, 1050 Brussels, Belgium., Sarret P; Institut de Pharmacologie de Sherbrooke, Department of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12e Avenue Nord, J1H 5N4 Sherbrooke, Quebec, Canada., Ballet S; Research Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel, 1050 Brussels, Belgium. |
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Jazyk: | angličtina |
Zdroj: | ACS pharmacology & translational science [ACS Pharmacol Transl Sci] 2024 Aug 19; Vol. 7 (9), pp. 2784-2798. Date of Electronic Publication: 2024 Aug 19 (Print Publication: 2024). |
DOI: | 10.1021/acsptsci.4c00236 |
Abstrakt: | Linking an opioid to a nonopioid pharmacophore represents a promising approach for reducing opioid-induced side effects during pain management. Herein, we describe the optimization of the previously reported opioid-neurotensin hybrids (OPNT-hybrids), SBL-OPNT-05 & -10 , containing the μ-/δ-opioid agonist H-Dmt-d-Arg-Aba-β-Ala-NH Competing Interests: The authors declare no competing financial interest. (© 2024 American Chemical Society.) |
Databáze: | MEDLINE |
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