Inhibitory effect of epinastine on superoxide generation by rat neutrophils.
We studied the effects of antiallergic drugs, epinastine, ketotifen, oxatomide, mequitazine and cromolyn sodium on superoxide anion (O2-) generation from rat neutrophils. Epinastine, ketotifen, oxatomide and mequitazine dose-dependently prevented the N-formyl-Met-Leu-Phe- and phorbol 12-myristate 13-acetate-induced O2- generation, but cromolyn sodium did not prevent it. When membrane and cytosol fractions were incubated with each drug, epinastine, ketotifen and mequitazine prevented O2- generation. On the other hand, when only the membrane fraction was incubated with each drug, ketotifen and mequitazine prevented O2- generation, but epinastine did not. Epinastine may inhibit the NADPH oxidase system through the obstruction of NADPH oxidase-associated cytosol components.
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Japan.
N
N
Fukuishi
T
T
Kan
K
K
Hirose
R
R
Akagi
M
M
Akagi
D000818:Animals; D018926:Anti-Allergic Agents / Q000494:pharmacology*; D003984:Dibenzazepines / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007093:Imidazoles / Q000494:pharmacology*; D007665:Ketotifen / Q000494:pharmacology; D008297:Male; D009247:NADH, NADPH Oxidoreductases / Q000187:drug effects; D019255:NADPH Oxidases; D009504:Neutrophils / Q000187:drug effects*; D010879:Piperazines / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013481:Superoxides / Q000378:metabolism*
D018926:Anti-Allergic Agents; D003984:Dibenzazepines; D007093:Imidazoles; D010879:Piperazines; D013481:Superoxides; D009247:NADH, NADPH Oxidoreductases; D019255:NADPH Oxidases; C015408:oxatomide; C053090:epinastine; D007665:Ketotifen