Effect of the new anti-allergic compound ethyl 2-(4'-carboxybenzamido)-4-propionamidobenzoate sodium salt on human neutrophil superoxide production.
The effect of the new orally active antiallergic compound ethyl 2-(4'-carboxybenzamido)-4-propionamidobenzoate sodium salt (AM-682) and its main metabolite (met-A) were evaluated on respiratory burst in isolated human polymorphonuclear neutrophils (PMN). Both compounds exhibited inhibitory effect with concentration dependency on the n-formyl-methionyl-leucyl-phenylalanine (FMLP)-induced superoxide (O-2) production by human PMN. The inhibitory activity of met-A (IC50 1.1 mumol/l) was higher than that of AM-682 (IC50 85 mumol/l). By contrast, these compounds affected neither PMN O-2 production induced by phorbol 12-myristate 13-acetate (PMA) nor extracellular O-2 generation by the reaction of xanthine oxidase with hypoxanthine. These results indicate that the effects of these compounds act specifically on the generation of O-2 and is not simply a scavenger of O-2. This anti-inflammatory effect may also be beneficial in the treatment of asthma.
Kaneko
M
M
2nd Department of Internal Medicine, Nagoya University School of Medicine, Japan.
Suzuki
K
K
Furui
H
H
Takagi
K
K
Satake
T
T
D000328:Adult; D062365:Aminobenzoates / Q000494:pharmacology*; D001549:Benzamides / Q000494:pharmacology*; D003574:Cytochrome c Group / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism*; D010084:Oxidation-Reduction; D010101:Oxygen Consumption / Q000187:drug effects; D013481:Superoxides / Q000378:metabolism*; D062366:para-Aminobenzoates
D062365:Aminobenzoates; D001549:Benzamides; D003574:Cytochrome c Group; D062366:para-Aminobenzoates; D013481:Superoxides; C063927:ethyl 2-(4'-carboxybenzamido)-4-propionamidobenzoate; C063928:ethyl 2-(4'-carboxybenzamido)-4-aminobenzoate