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Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2007 Nov 29; Vol. 50 (24), pp. 5882-5. Date of Electronic Publication: 2007 Oct 27. - Publication Year :
- 2007
-
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.
- Subjects :
- Adamantane pharmacology
Animals
Benzamides pharmacology
Blood Proteins metabolism
Crystallography, X-Ray
Humans
In Vitro Techniques
Molecular Conformation
Monocytes metabolism
Protein Binding
Rats
Receptors, Purinergic P2X7
Structure-Activity Relationship
Adamantane analogs & derivatives
Adamantane chemical synthesis
Benzamides chemical synthesis
Interleukin-1beta antagonists & inhibitors
Purinergic P2 Receptor Antagonists
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 50
- Issue :
- 24
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 17963373
- Full Text :
- https://doi.org/10.1021/jm700949w