1. TYB-2285 (1-30 mg/kg PO) inhibited ovalbumin (OA)- and dinitropheny
l-ascaris (DNPAs)-induced passive cutaneous anaphylaxis (PCA) in a dos
e dependent manner. 2. The ED(50) of TYB-2285 and ketotifen fumarate o
n OA induced PCA were 0.5 and 3.9 mg/kg, respectively. The ED(50) Of T
YP-2285 and amlexanox on DNP-As-induced PCA were 3,5 and 0.9mg/ kg, re
spectively. 3. TYB-2285 (3-30 mg/kg PO) inhibited histamine consumptio
n at the PCA site. 4. Unlike cyproheptadine or amlexanox, TYB 2285 (30
mg/kg PO) did not inhibit histamine-, se rotonin-, ascites-, 48/80-,
or A23187-induced capillary permeability. It inhibited dextran-induced
capillary permeability slightly. 5. These results demonstrate that TY
B-2285 inhibits PCA by inhibiting histamine release, although it does
not inhibit capillary permeabilty. Copyright (C) 1997 Elsevier Science
Inc.