4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective δ-opioid agonists
| Autor: | Andrés A. Trabanco, Rosa M. Alvarez, Frans Eduard Janssens, Thomas Steckler, Inge Boeckx, Theo F. Meert, Laura Iturrino, Leenaerts Joseph Elisabeth, Antonio Gómez, Encarna Matesanz, Shirley Pullan, Ana Isabel de Lucas, Javier Fernández, J. Alonso, José Ignacio Andrés |
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| Rok vydání: | 2006 |
| Předmět: |
Agonist
Drug Industry Stereochemistry medicine.drug_class Clinical Biochemistry GTPgammaS Pharmaceutical Science Binding Competitive Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Piperidines Receptors Opioid delta Drug Discovery medicine Receptor Molecular Biology Organic Chemistry Imidazoles Affinities In vitro Kinetics Models Chemical chemistry Opioid Drug Design Molecular Medicine Peptides Selectivity medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 16:146-149 |
| ISSN: | 0960-894X |
| Popis: | A novel series of 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives has been prepared and their synthesis described herein. In vitro affinities for delta-, mu-, and kappa-opioid receptors, as well as the functional activity in the [(35)S]GTPgammaS assay are reported. The most potent and selective delta-opioid agonist 18a exhibited a K(i) of 18 nM, and was >258-fold and 28-fold selective over mu- and kappa-receptors, respectively; the compound is a full agonist with an EC(50) value of 14 nM. |
| Databáze: | OpenAIRE |
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