e-6123 and Anaphylaxis

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 micrograms/kg, respectively. E6123 inhibited Ag inhalation-induced airway hyperreactivity in guinea pigs after oral administration at 30 micrograms/kg. E6123 protected mice from anaphylactic death with an ED50 value (p.o.) of 7 micrograms/kg. The inhibitory effects of E6123 described above were very potent compared to 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.

Topics: Administration, Inhalation; Anaphylaxis; Animals; Antigens; Asthma; Azepines; Guinea Pigs; Male; Mice; Mice, Inbred ICR; Ovalbumin; Platelet Activating Factor; Propranolol; Pyrilamine; Triazoles

E6123 inhibited antigen-induced bronchoconstriction, the development of bronchial hyperreactivity and eosinophil infiltration in the airway in passively sensitized guinea pigs and protected mice from anaphylactic death. The inhibitory effects of E6123 on anaphylactic response were very potent compared with those of WEB 2347 and Y-24180.

Topics: Anaphylaxis; Animals; Antigens; Azepines; Bronchoconstriction; Guinea Pigs; Male; Mice; Mice, Inbred ICR; Platelet Activating Factor; Platelet Aggregation; Triazoles