Abstract
A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease.
MeSH terms
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Adamantane / analogs & derivatives*
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Adamantane / chemical synthesis*
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Adamantane / pharmacology
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Animals
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Benzamides / chemical synthesis*
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Benzamides / pharmacology
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Blood Proteins / metabolism
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Crystallography, X-Ray
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Humans
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In Vitro Techniques
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Interleukin-1beta / antagonists & inhibitors*
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Molecular Conformation
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Monocytes / metabolism
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Protein Binding
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Purinergic P2 Receptor Antagonists*
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Rats
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Receptors, Purinergic P2X7
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Structure-Activity Relationship
Substances
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Benzamides
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Blood Proteins
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Interleukin-1beta
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P2RX7 protein, human
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P2rx7 protein, rat
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Purinergic P2 Receptor Antagonists
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Receptors, Purinergic P2X7
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Adamantane