Arylacetamide kappa-selective opioid ligands
Autor: | Anthony D. Pechulis, Jean M. Bidlack, Sydney Archer, Mark P. Wentland, Ann M. Colasurdo |
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Rok vydání: | 1997 |
Předmět: |
medicine.drug_class
Stereochemistry Ligand Organic Chemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis chemistry.chemical_compound chemistry Opioid Opioid receptor Drug Discovery medicine Molecular Medicine Amine gas treating Enantiomer Molecular Biology Acetamide medicine.drug |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 7:2271-2276 |
ISSN: | 0960-894X |
DOI: | 10.1016/s0960-894x(97)00406-x |
Popis: | A family of arylacetamide opioid ligands was prepared. Competition binding studies indicate that in each case the (S)-(+) series was two orders of magnitude more potent than the corresponding (R)-(−) series and that the amine (S)-(+)- 3 and the acetamide (S)-(+)- 4 were selective for the κ opioid binding site. Binding and flow cytometry experiments demonstrated that (S)-(+)-FITC-AA 5 was the enantiomer that bound to the κ opioid receptor. |
Databáze: | OpenAIRE |
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