Synthesis and evaluation of 2-amido-3-carboxamide thiophene CB2 receptor agonists for pain management
| Autor: | B B Yao, William A. Carroll, Jennifer M. Frost, Madhavi Pai, George K. Grayson, Chang Zhu, Bradley A. Hooker, Alan S. Florjancic, Karin R. Tietje, Michael Meyer, Anthony V. Daza, Michael J. Dart, Tiffany Runyan Garrison, Derek W. Nelson, Keith B. Ryther, Gin C. Hsieh, Prasant Chandran, Odile F. El-Kouhen, Yihong Fan |
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| Rok vydání: | 2012 |
| Předmět: |
medicine.drug_class
Stereochemistry medicine.medical_treatment Organic Chemistry Clinical Biochemistry Antagonist Pharmaceutical Science Carboxamide Pharmacology Biochemistry Radioligand Assay chemistry.chemical_compound chemistry Drug Discovery Thiophene medicine Cannabinoid receptor type 2 Molecular Medicine Structure–activity relationship Cannabinoid Molecular Biology ADME |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 22:2604-2608 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2012.01.121 |
| Popis: | SAR studies on a series of thiophene amide derivatives provided CB(2) receptor agonists. The activity of the compounds was characterized by radioligand binding determination, multiple functional assays, ADME, and pharmacokinetic studies. A representative compound with selectivity for CB(2) over CB(1) effectively produced analgesia in behavioral models of neuropathic, inflammatory, and postsurgical pain. Control experiments using a CB(2) antagonist demonstrated the efficacy in the pain models resulted from CB(2) agonism. |
| Databáze: | OpenAIRE |
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