Abstract

The effects of the platelet-activating factor (PAF) antagonist, E6123, on anaphylactic responses in guinea pigs and mice were investigated. E6123 inhibited i.v. antigen (Ag)- or inhaled Ag-induced bronchoconstriction in passively and actively sensitized guinea pigs after oral administration at 3 and 10 μg/kg, respectively. E6123 inhibited Ag inhalation-induced airway hyperreactivity in guinea pigs after oral administration of 30 μg/kg. E6123 protected mice from anaphylactic death with an ED50 value (p.o.) of 7 μg/kg. The inhibitory effects of E6123 described above were very potent compared t those of the PAF-antagonists WEB2347 and Y-24180.The present results suggest that E6123 may be beneficial for the treatment of asthma, a condition in which PAF is assumed to be involved.

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