Literature DB >> 14592504

Novel P2X7 receptor antagonists.

L Alcaraz1, A Baxter, J Bent, K Bowers, M Braddock, D Cladingboel, D Donald, M Fagura, M Furber, C Laurent, M Lawson, M Mortimore, M McCormick, N Roberts, M Robertson.   

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.

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Year:  2003        PMID: 14592504     DOI: 10.1016/j.bmcl.2003.08.033

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  18 in total

1.  C-terminal calmodulin-binding motif differentially controls human and rat P2X7 receptor current facilitation.

Authors:  Sébastien Roger; Ludovic Gillet; Alberto Baroja-Mazo; Annmarie Surprenant; Pablo Pelegrin
Journal:  J Biol Chem       Date:  2010-04-08       Impact factor: 5.157

2.  Identification of Thr283 as a key determinant of P2X7 receptor function.

Authors:  M T Young; P Pelegrin; A Surprenant
Journal:  Br J Pharmacol       Date:  2006-08-29       Impact factor: 8.739

Review 3.  Pharmacology of P2X channels.

Authors:  Joel R Gever; Debra A Cockayne; Michael P Dillon; Geoffrey Burnstock; Anthony P D W Ford
Journal:  Pflugers Arch       Date:  2006-04-29       Impact factor: 3.657

4.  Negative and positive allosteric modulators of the P2X(7) receptor.

Authors:  A D Michel; L J Chambers; D S Walter
Journal:  Br J Pharmacol       Date:  2007-12-10       Impact factor: 8.739

5.  Adenosine diphosphate involvement in THP-1 maturation triggered by the contact allergen 1-fluoro-2,4-dinitrobenzene.

Authors:  J D Martins; A Silva; I Ferreira; M Gonçalo; J B A Custódio; M C Lopes; M R M Domingues; B M Neves; M T Cruz
Journal:  Toxicol Res (Camb)       Date:  2016-08-04       Impact factor: 3.524

Review 6.  Roles of P2X7 receptor in glial and neuroblastoma cells: the therapeutic potential of P2X7 receptor antagonists.

Authors:  Synthia H Sun
Journal:  Mol Neurobiol       Date:  2010-04-21       Impact factor: 5.590

Review 7.  Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states.

Authors:  D L Donnelly-Roberts; M F Jarvis
Journal:  Br J Pharmacol       Date:  2007-04-30       Impact factor: 8.739

8.  Reanalysis of P2X7 receptor expression in rodent brain.

Authors:  Joan A Sim; Mark T Young; Hye-Youn Sung; R Alan North; Annmarie Surprenant
Journal:  J Neurosci       Date:  2004-07-14       Impact factor: 6.167

9.  Identification and characterization of a novel variant of the human P2X(7) receptor resulting in gain of function.

Authors:  Chengqun Sun; Jessica Chu; Sarita Singh; Russell D Salter
Journal:  Purinergic Signal       Date:  2009-10-17       Impact factor: 3.765

10.  Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor.

Authors:  Ga Eun Lee; Bhalchandra V Joshi; Wangzhong Chen; Lak Shin Jeong; Hyung Ryong Moon; Kenneth A Jacobson; Yong-Chul Kim
Journal:  Bioorg Med Chem Lett       Date:  2007-11-28       Impact factor: 2.823

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