The antiallergic activities of synthetic acrophylline [1] and acrophyllidine [2] have been demonstrated. Both compounds 1 and 2 at 30 mu mol/kg reduced the plasma leakage in mouse ear in a passive cutaneous anaphylactic (PCA) reaction. In addition, compound 1 suppressed mast cell degranulation in a dose-dependent manner, while compound 2 at 100 mu M produced no significant inhibition of the release of preformed inflammatory mediators. These results suggest that the antiallergic effect of compound I probably occurs through the suppression of mast cell degranulation, and that of compound 2 by protection of the vasculature against challenge by mediators of inflammation.