Effectiveness of MY-5116 against Allergic Rhinitis
1987 Volume 1987 Issue Supplement18 Pages 1-14
Details
1987 Volume 1987 Issue Supplement18 Pages 1-14
MY-5116 is a newly synthesized antiallergic agent and the metabolite, of which MY-1250, inhibits the release of chemical mediators from mast cells in animals.
This paper describes the inhibitory effect of MY-1250 on the release of histamine and SRS-A from allergen-stimulated human basophils collected from patients with al- lergic rhinitis induced by the pollen of Cryptomeria Japonica D. Don (PCJ). Basophils purified from a donor's peripheral blood were passively sensitized with the same donor's reaginic serum containing anti-PCJIgE class antibodies (aPCJIgEAb).
1) Added before antigen stimulation, MY-1250 produced a dose dependent inhibition with an ED50 10-8-10-8g/ml of specific antigen (PCJ) induced histamine and SRS-A release from human peripheral basophils passively sensitized with aPCJ-IgEAb.
2) MY-1250 also inhibited Ca2+ ior. ophore A23187 induced histamine and SRS-A release from non passively sensitized human peripheral basophils in a dose dependent manner when added to these cells before A23187 stimulation.
3) It has been reported that the oral administration of 150 mg of MY-5116 in humans gives a maximum plasma MY-1250 level of 1.5×10-8g/ml. Considering the in vitro efficacy of MY-1250 in this experiment and the reported human plasma. level, MY-5116 should be a useful prophylactic drug for various type I allergic diseases, including allergic rhinitis.
