Abstract
C-3 Amido-indoles were found to selectively bind to the CB2 receptor. SAR studies led to optimized compounds with excellent in vivo potency against LPS induced TNF-alpha release in murine models of cytokine production.
MeSH terms
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Amides
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Animals
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Anti-Inflammatory Agents / chemical synthesis*
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Anti-Inflammatory Agents / pharmacology
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Cell Line
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Humans
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Immunity, Cellular / drug effects
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Indoles
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Inhibitory Concentration 50
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Leukocytes, Mononuclear / drug effects
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Leukocytes, Mononuclear / metabolism
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Lipopolysaccharides / pharmacology
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Mice
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Protein Binding
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Receptors, Cannabinoid
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Receptors, Drug / agonists*
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Sensitivity and Specificity
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Structure-Activity Relationship
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Tumor Necrosis Factor-alpha / antagonists & inhibitors
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Tumor Necrosis Factor-alpha / metabolism
Substances
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Amides
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Anti-Inflammatory Agents
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Indoles
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Lipopolysaccharides
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Receptors, Cannabinoid
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Receptors, Drug
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Tumor Necrosis Factor-alpha