作者:L. Alcaraz、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
DOI:10.1016/j.bmcl.2003.08.033
日期:2003.11
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. (C) 2003 Elsevier Ltd. All rights reserved.