[HTML][HTML] Identification of a potent and orally active non-peptide C5a receptor antagonist

H Sumichika, K Sakata, N Sato, S Takeshita… - Journal of Biological …, 2002 - ASBMB
The anaphylatoxin C5a is a potent chemotactic factor for neutrophils and other leukocytes,
and functions as an important inflammatory mediator. Through a high capacity screening
followed by chemical optimization, we identified a novel non-peptide C5a receptor
antagonist, N-[(4-dimethylaminophenyl) methyl]-N-(4-isopropylphenyl)-7-methoxy-1, 2, 3, 4-
tetrahydronaphthalen-1-carboxamide hydrochloride (W-54011). W-54011 inhibited the
binding of 125 I-labeled C5a to human neutrophils with aK i value of 2.2 nm. W-54011 also …