Discovery of Potent and Selective Adamantane-Based Small-Molecule P2X7 Receptor Antagonists/Interleukin-1β Inhibitors

Mark Furber,Lilian Alcaraz,Janice Bent,Armin Beyerbach,Keith Bowers,Martin Braddock,Moya Caffrey,David Cladingboel,John Collington,David Keith Donald,Malbinder Fagura,Frank Ince,Elizabeth Kinchin,Céline Laurent,Mandy Lawson,Timothy Jon Luker,Michael Mortimore,Austen Pimm,Robert J. Riley,Nicola J. Roberts,Mark J. Robertson,Jill Theaker,Philip Thorne,Richard Weaver,Peter J. H. Webborn,Paul Willis

Discovery of Potent and Selective Adamantane-Based Small-Molecule P2X7 Receptor Antagonists/Interleukin-1β Inhibitors

2007

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.

Keywords:

Adamantane
Small molecule
Interleukin
Organic chemistry
Biochemistry
Carboxamide
Receptor
Chemistry
interleukin 1β
p2x7 receptor
Antagonist
Chemical synthesis
In vitro

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