Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at μ and δ opioid receptors
| Autor: | Peg Davis, Josephine Lai, Richard S. Agnes, Yeon Sun Lee, Victor J. Hruby, Sharif Moye, Shou Wu Ma, Ruben Vardanyan, Frank Porreca, Joel Nyberg |
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| Rok vydání: | 2007 |
| Předmět: |
Agonist
Stereochemistry medicine.drug_class Clinical Biochemistry Receptors Opioid mu Pharmaceutical Science Ligands Transfection Biochemistry Article Cell Line δ-opioid receptor Structure-Activity Relationship chemistry.chemical_compound Piperidines Receptors Opioid delta Drug Discovery medicine Animals Humans Structure–activity relationship Receptor Molecular Biology chemistry.chemical_classification Analgesics Dipeptide Molecular Structure Organic Chemistry Amino acid chemistry Opioid Molecular Medicine μ-opioid receptor Muscle Contraction Protein Binding medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 17:2161-2165 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2007.01.114 |
| Popis: | New 4-anilidopiperidine analogues in which the phenethyl group of fentanyl was replaced by several aromatic ring-contained amino acids (or acids) were synthesized to study the biological effect of the substituents on mu and delta opioid receptor interactions. These analogues showed broad (47 nM-76 microM) but selective (up to 17-fold) binding affinities at the mu opioid receptor over the delta opioid receptor, as predicted from the message-address concept. |
| Databáze: | OpenAIRE |
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