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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Veröffentlicht in:	Journal of medicinal chemistry 2007-11, Vol.50 (24), p.5882-5885
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	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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Beschreibung
Zusammenfassung:	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