Bepotastine Besilate

Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. (In Vitro) :Bepotastine besilate (10, 100, 1000 μM; preincubates for 120 min) decreases the release of histamine induced by A23187 treatment, which reaches a statistically significant reduces level at 1000 μM.Bepotastine besilate (50 μM; 1 h) suppresses the expression of NGF mRNA in NHEKs. (In Vivo) :Bepotastine besilate (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) demonstrates significant inhibition of PAF-induced conjunctival eosinophil infiltration.Bepotastine besilate (3 mg/kg; p.o.; once) suppresses scratching behavior to a frequency of 59.0 and a duration of 14.57 seconds, which are almost the same levels compares with the control.Bepotastine besilate (10 mg/kg; p.o.; once) significantly suppresses serum LTB 4 levels to 711.3 pg/mL at 1 h and 858.8 pg/mL at 2 h in NC/Nga mice with a rash.