Abstract
The synthesis and pharmacological evaluation of a new series of potent P2X(7) receptor antagonists is disclosed. The compounds inhibit BzATP-mediated pore formation in THP-1 cells. The distribution of the P2X(7) receptor in inflammatory cells, most notably the macrophage, mast cell and lymphocyte, suggests that P2X(7) antagonists have a significant role to play in the treatment of inflammatory disease.
MeSH terms
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Adenosine Triphosphate / analogs & derivatives*
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Adenosine Triphosphate / chemical synthesis*
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Adenosine Triphosphate / pharmacology
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Cell Line
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Humans
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Kinetics
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Molecular Structure
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Purinergic P2 Receptor Antagonists*
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Receptors, Purinergic P2X7
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Structure-Activity Relationship
Substances
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P2RX7 protein, human
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Purinergic P2 Receptor Antagonists
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Receptors, Purinergic P2X7
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3'-O-(4-benzoyl)benzoyladenosine 5'-triphosphate
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Adenosine Triphosphate