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A. Fujii, T. Kida, H. Sakaki; Comparison of the Inhibitory Effects of Bepotastine Besilate and Other H1 Receptor Antagonists on Histamine Release From Mast Cells and Chemotaxis of Eosinophils. Invest. Ophthalmol. Vis. Sci. 2009;50(13):6315.
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Bepotastine besilate (Bepo) is a highly selective histamine H1 receptor antagonist and also stabilizes mast cells and decreases eosinophil infiltration. In this study, the inhibitory effects of Bepo on histamine release in vitro from rat peritoneal mast cells and on chemotaxis of guinea pig peritoneal eosinophils were compared with inhibition by other ophthalmic H1 antagonists: ketotifen fumarate (Keto) and olopatadine hydrochloride (Olop).
Mast cells which were isolated from rat peritoneal cells were pre-incubated with each H1 antagonist for 120 min, the calcium ionophore A23187 was added, and the cells were incubated further 10 min at 37°C. The histamine contents in culture media then were measured by ELISA (IBL-Hamburg). Separately, eosinophils isolated from guinea pig peritoneal cells were pre-incubated with each H1 antagonist for 20 min, placed in upper wells of microchemotaxis chamber slides (Neuro Probe), and incubated with leukotriene B4 (LTB4) as a chemoattractant in lower wells for 90 min at 37°C. The eosinophils migrating towards lower wells were stained with Giemsa and counted.
Bepo inhibited A23187-induced histamine release from mast cells at 1 mM (statistically significant p<0.01). Keto inhibited at only 0.1 mM, while its effect was attenuated at 1 mM. Olop did not inhibit histamine release up to 1 mM.Both Bepo and Keto dose-dependently inhibited LTB4-induced chemotaxis of eosinophils at 0.1 mM (% of control: 81.4% and 79.3%, respectively) and 1 mM (30.7% and 1.8%). Chemotaxis was only slightly inhibited by Olop at 1 mM (68.5%). After incubation with 1 mM Keto but not 1 mM Bepo, cell injury of eosinophils was observed.
The inhibitory effects of Bepo and Keto on histamine release from isolated mast cells and eosinophil chemotaxis were more potent than Olop. These findings suggest that Bepo has potential to attenuate allergic inflammation with a favorable safety profile and could be a useful ophthalmic H1 antagonist.
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