Direct effects of second-generation H1-receptor antagonists on the activation of human basophils

The present study was performed to investigate the putative suppressive effects of H₁-receptor antagonists (HRA) of the second generation (astemizole (AS), cetirizine (CT), loratadine (LO), oxatomide (OX) and terfenadine (TF)) on the mediator release from human basophils activated by two classical stimuli. Anti-IgE-mediated histamine release was inhibited in a dose-dependent fashion by TF (maximum inhibitory value: 33.8±7.6%, 100 μM,n=7), whereas the other HRA exhibited weaker activity. The anti-IgE-induced LTC₄ production was strongly suppressed by TF, LO and OX (92.4±6.3%, 90.8±6.0% and 88.5±5.6%, 100 μM,n=4−5), while As was less active (56.4±4.1%, 100 μM,n=5). Histamine release induced by incubation with grass pollen antigen (0.01%) was inhibited by TF (40.7±4.1%, 50 μM,n=4), but the other HRA showed only low activity. The present findings suggest that some HRA might exhibit direct inhibitory effects on activation of IgE-receptor bearing cells.