Identification of a Selective Nonpeptide Antagonist of the Anaphylatoxin C3a Receptor That Demonstrates Antiinflammatory Activity in Animal Models

The anaphylatoxin C3a is a potent chemotactic peptide and inflammatory mediator released during complement activation which binds to and activates a G-protein-coupled receptor. Molecular cloning of the C3aR has facilitated studies to identify nonpeptide antagonists of the C3aR. A chemical lead that...

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Veröffentlicht in:	The Journal of immunology (1950) 2001-05, Vol.166 (10), p.6341-6348
Hauptverfasser:	Ames, Robert S, Lee, Dennis, Foley, James J, Jurewicz, Anthony J, Tornetta, Mark A, Bautsch, Wilfried, Settmacher, Britta, Klos, Andreas, Erhard, Karl F, Cousins, Russell D, Sulpizio, Anthony C, Hieble, J. Paul, McCafferty, Gerald, Ward, Keith W, Adams, Jerry L, Bondinell, William E, Underwood, David C, Osborn, Ruth R, Badger, Alison M, Sarau, Henry M
Format:	Artikel
Sprache:	eng
Schlagworte:	anaphylatoxin C3a anaphylatoxin C3a receptors Animals Anti-Inflammatory Agents, Non-Steroidal - metabolism Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics Anti-Inflammatory Agents, Non-Steroidal - pharmacology Arginine - analogs & derivatives Arginine - metabolism Arginine - pharmacokinetics Arginine - pharmacology Arthritis, Experimental - immunology Arthritis, Experimental - pathology Benzhydryl Compounds - metabolism Benzhydryl Compounds - pharmacokinetics Benzhydryl Compounds - pharmacology Binding, Competitive Cell Line Complement C3a - metabolism Complement Inactivator Proteins - metabolism Complement Inactivator Proteins - pharmacokinetics Complement Inactivator Proteins - pharmacology Disease Models, Animal Edema - pathology Edema - prevention & control Guinea Pigs Hindlimb Humans Injections, Intraperitoneal Leukocytosis - immunology Leukocytosis - pathology Male Membrane Proteins Mice Muscle Contraction - drug effects N-[(2,2-diphenylethoxy)acetyl]-L-arginine Neutrophil Infiltration - drug effects Rats Rats, Inbred Lew Rats, Sprague-Dawley Receptors, Complement - antagonists & inhibitors Receptors, Complement - metabolism Tumor Cells, Cultured
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