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1.
Novel P2X7 receptor antagonists.
Alcaraz, L; Baxter, A; Bent, J; Bowers, K; Braddock, M; Cladingboel, D; Donald, D; Fagura, M; Furber, M; Laurent, C; Lawson, M; Mortimore, M; McCormick, M; Roberts, N; Robertson, M.
Bioorg Med Chem Lett ; 13(22): 4043-6, 2003 Nov 17.
Article in English | MEDLINE | ID: mdl-14592504

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.


Subject(s)
Adenosine Triphosphate/analogs & derivatives , Adenosine Triphosphate/chemical synthesis , Purinergic P2 Receptor Antagonists , Adenosine Triphosphate/pharmacology , Cell Line , Humans , Kinetics , Molecular Structure , Receptors, Purinergic P2X7 , Structure-Activity Relationship
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