N,N-Diethyl-4-[(3-hydroxyphenyl)(piperidin-4-yl)amino] benzamide derivatives: The development of diaryl amino piperidines as potent δ opioid receptor agonists with in vivo anti-nociceptive activity in rodent models
| Autor: | Martin Coupal, Paul Jones, Lejla Hodzic, Wenhau Xiao, Edward Roberts, Andrew Griffin, Daniel Delorme, Dominic Salois, Maryse Labarre, Stephane St-Onge, Christopher Walpole, Jamie Boulet, Lars Gawell, Rico Lavoie, Joanne Butterworth, William Brown |
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| Rok vydání: | 2009 |
| Předmět: |
Agonist
Stereochemistry medicine.drug_class Clinical Biochemistry Analgesic Pharmaceutical Science Carboxamide Biochemistry κ-opioid receptor δ-opioid receptor Mice Structure-Activity Relationship chemistry.chemical_compound Piperidines In vivo Opioid receptor Receptors Opioid delta Drug Discovery medicine Animals Benzamide Molecular Biology Analgesics Chemistry Organic Chemistry Diphenylamine Rats Disease Models Animal Benzamides Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 19:5994-5998 |
| ISSN: | 0960-894X |
| Popis: | We have investigated a series of phenolic diaryl amino piperidine delta opioid receptor agonists, establishing the importance of the phenol functional group and substitution on the piperdine nitrogen for delta agonist activity and selectivity versus the mu and kappa opioid receptors. This study uncovered compounds with improved agonist potency and selectivity compared to the standard, non-peptidic delta agonist SNC-80. In vivo anti-nociceptive activity of analog 8e in two rodent models is discussed, demonstrating the potential of delta agonists to provide a novel mechanism for pain relief. |
| Databáze: | OpenAIRE |
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