Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors

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.

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Bibliographic Details
Published in:Journal of medicinal chemistry 2007-11, Vol.50 (24), p.5882-5885
Main Authors: Furber, Mark, Alcaraz, Lilian, Bent, Janice E, Beyerbach, Armin, Bowers, Keith, Braddock, Martin, Caffrey, Moya V, Cladingboel, David, Collington, John, Donald, David K, Fagura, Malbinder, Ince, Frank, Kinchin, Elizabeth C, Laurent, Celine, Lawson, Mandy, Luker, Timothy J, Mortimore, Michael M P, Pimm, Austen D, Riley, Robert J, Roberts, Nicola, Robertson, Mark, Theaker, Jill, Thorne, Philip V, Weaver, Richard, Webborn, Peter, Willis, Paul
Format: Article
Language:English
Subjects:
Adamantane - analogs & derivatives
Adamantane - chemical synthesis
Adamantane - pharmacology
Animals
Benzamides - chemical synthesis
Benzamides - pharmacology
Blood Proteins - metabolism
Crystallography, X-Ray
Humans
In Vitro Techniques
Interleukin-1beta - antagonists & inhibitors
Molecular Conformation
Monocytes - metabolism
Protein Binding
Purinergic P2 Receptor Antagonists
Rats
Receptors, Purinergic P2X7
Structure-Activity Relationship
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Description
Summary: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.
ISSN:0022-2623