Novel P2X7 receptor antagonists

descriptionPublicationkeyboard_double_arrow_right Article 01 Nov 2003 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 13, pages 4,043-4,046 (issn: 0960-894X,

Copyright policy )

Authors: L, Alcaraz; A, Baxter; J, Bent; K, Bowers; M, Braddock; D, Cladingboel; D, Donald; +8 Authors

doi: 10.1016/j.bmcl.2003.08.033

pmid: 14592504

Novel P2X7 receptor antagonists

- Summary
- Subjects
- Metrics

Abstract

The synthesis and pharmacological evaluation of a new series of potent P2X(7) receptor antagonists is disclosed. The compounds inhibit BzATP-mediated pore formation in THP-1 cells. The distribution of the P2X(7) receptor in inflammatory cells, most notably the macrophage, mast cell and lymphocyte, suggests that P2X(7) antagonists have a significant role to play in the treatment of inflammatory disease.

Related Organizations

AstraZeneca (United Kingdom)
United Kingdom
Loughborough University
United Kingdom

Keywords

Kinetics, Structure-Activity Relationship, Adenosine Triphosphate, Molecular Structure, Purinergic P2 Receptor Antagonists, Humans, Receptors, Purinergic P2X7, Cell Line

Impact byBIP!

	selected citations These citations are derived from selected sources. This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).	59
	popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.	Top 10%
	influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).	Top 10%
	impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.	Top 10%