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

Autor:	Mark Furber, Cladingboel David, Janice Bent, M.J. Robertson, Timothy Jon Luker, Lilian Alcaraz, Michael Mortimore, Moya Caffrey, Martin Braddock, Robert J. Riley, Celine Laurent, Peter J. H. Webborn, Frank Ince, Philip Thorne, Jill Theaker, John Collington, Elizabeth Kinchin, Mandy Lawson, Austen Pimm, Armin Beyerbach, Richard J. Weaver, Keith Bowers, David Donald, Malbinder Fagura, Paul Willis, Nicola Roberts
Rok vydání:	2007
Předmět:	medicine.drug_class Adamantane Interleukin-1beta Molecular Conformation Carboxamide In Vitro Techniques Crystallography X-Ray Chemical synthesis Monocytes chemistry.chemical_compound Structure-Activity Relationship Drug Discovery medicine Purinergic P2 Receptor Antagonists Animals Humans P2x7 receptor Antagonist Blood Proteins Small molecule In vitro Rats Interleukin 1β Biochemistry chemistry Benzamides Molecular Medicine Receptors Purinergic P2X7 Protein Binding
Zdroj:	Journal of medicinal chemistry. 50(24)
ISSN:	0022-2623
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::686eb5727d8f1e1a68fedd60a58958c3 https://pubmed.ncbi.nlm.nih.gov/17963373 Zobrazit plný text záznamu