Abstract
Further on to our earlier work on the 4-oxo-1,4-dihydropyridine, we describe herein our strategy to get access to potent selective CB₂ receptor agonists. Thus, we designed and synthesized 29 compounds, evaluated on both hCB₁ and hCB₂ cannabinoid receptors, and assessed 11 of them in the TNBS-induced colitis model in mice. Compound 48 was found to be the most efficient of our series, exhibiting an exquisite protection against experimental colitis, superior to the one observed after treatment with Pentasa.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adamantane / analogs & derivatives*
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Adamantane / chemical synthesis*
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Adamantane / chemistry
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Adamantane / pharmacology
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Binding, Competitive
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Blood Proteins / metabolism
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CHO Cells
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Colitis / chemically induced
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Colitis / pathology
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Colitis / prevention & control*
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Cricetinae
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Cricetulus
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Humans
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Intestinal Absorption
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Ligands
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Mice
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Microsomes, Liver / metabolism
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Protein Binding
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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Radioligand Assay
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Receptor, Cannabinoid, CB2 / agonists*
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Structure-Activity Relationship
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Trinitrobenzenesulfonic Acid
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Blood Proteins
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Ligands
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Pyridines
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Receptor, Cannabinoid, CB2
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Trinitrobenzenesulfonic Acid
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Adamantane