Bepotastine

Bepotastine is an antagonist of the histamine H₁ receptor that is selective over H₃, α₁-, α₂-, and β-adrenergic, dopamine D_2long, serotonin 5-HT₂, muscarinic acetylcholine, and benzodiazepine receptors.¹ It reduces dye leakage from the nasal passages of rats acutely sensitized to an antigen (ED₅₀ = 0.03 mg/kg) and inhibits histamine-induced bronchoconstriction in the anesthetized dog (ED₅₀ = 3.2 ?g/kg).^2,3 Bepotastine prevents conjunctival vascular hyperpermeability in a guinea pig model of conjunctivitis in a dose-dependent manner.⁴ Formulations containing bepotastine have been used in the treatment of itching associated with allergic conjunctivitis.

1.Kato, M., Nishida, A., Aga, Y., et al.Pharmacokinetic and pharmacodynamic evaluation of central effect of the novel antiallergic agent betotastine besilate.Arzneimittelforschung.47(10)1116-1124(1997) 2.Murata, T., Matsumoto, Y., Suzuki, T., et al.Effect of betotastine besilate (TAU-284), a novel anti-allergic agent, on experimental allergic rhinitisArerugi46(7)576-584(1997) 3.Matsubara, S., Ono, C., Yamazaki, N., et al.Inhibitory effects of bepotastine, a novel anti-allergic drug on histamine-induced bronchoconstriction in anesthetized dogsYakuri to Chiryo25(4)895-900(1997) 4.Kida, T., Fuji, A., Sakai, O., et al.Bepotastine besilate, a highly selective histamine H1 receptor antagonist, suppresses vascular hyperpermeability and eosinophil recruitment in in vitro and in vivo experimental allergic conjunctivitis modelsExp. Eye Res.91(1)85-91(2010)