| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369981 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
SAR studies on a series of thiophene amide derivatives provided CB2 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 CB2 over CB1 effectively produced analgesia in behavioral models of neuropathic, inflammatory, and postsurgical pain. Control experiments using a CB2 antagonist demonstrated the efficacy in the pain models resulted from CB2 agonism.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Derek W. Nelson, Jennifer M. Frost, Karin R. Tietje, Alan S. Florjancic, Keith Ryther, William A. Carroll, Michael J. Dart, Anthony V. Daza, Bradley A. Hooker, George K. Grayson, Yihong Fan, Tiffany R. Garrison, Odile F. El-Kouhen, Betty Yao,