Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371154 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
Abstract
A novel series of decahydroquinoline CB2 agonists is described. Optimization of the amide substituent led to improvements in CB2/CB1 selectivity as well as physical properties. Two key compounds were examined in the rat CFA model of acute inflammatory pain. A moderately selective CB2 agonist was active in this model. A CB2 agonist lacking functional CB1 activity was inactive in this model despite high in vivo exposure both peripherally and centrally.
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Organic Chemistry
Authors
Peter J. Manley, Amy Zartman, Daniel V. Paone, Christopher S. Burgey, Darrell A. Henze, Kimberly Della Penna, Reshma Desai, Michael D. Leitl, Wei Lemaire, Rebecca B. White, Suzie Yeh, Mark O. Urban, Stefanie A. Kane, George D. Hartman, Mark T. Bilodeau,